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enalaprilat anhydrous

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Description

Enalaprilat: The active metabolite of ENALAPRIL and one of the potent, intravenously administered, ANGIOTENSIN-CONVERTING ENZYME INHIBITORS. It is an effective agent for the treatment of essential hypertension and has beneficial hemodynamic effects in heart failure. The drug produces renal vasodilation with an increase in sodium excretion. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

enalaprilat dihydrate : The dihydrate form of enalaprilat, an angiotensin-converting enzyme (ACE) inhibitor that is used (often in the form of its prodrug, enalapril) in the treatment of hypertension and heart failure, for reduction of proteinuria and renal disease in patients with nephropathies, and for the prevention of stroke, myocardial infarction, and cardiac death in high-risk patients. Unlike enalapril, enalaprilat is not absorbed by mouth but is administered by intravenous injection. [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]

enalaprilat (anhydrous) : Enalapril in which the ethyl ester group has been hydrolysed to the corresponding carboxylic acid. Enalaprilat is an angiotensin-converting enzyme (ACE) inhibitor and is used (often in the form of its prodrug, enalapril) in the treatment of hypertension and heart failure, for reduction of proteinuria and renal disease in patients with nephropathies, and for the prevention of stroke, myocardial infarction, and cardiac death in high-risk patients. Unlike enalapril, enalaprilat is not absorbed by mouth but is given by intravenous injection, usually as the dihydrate. [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 CID5462501
CHEBI ID4786
SCHEMBL ID37289
MeSH IDM0329455

Synonyms (90)

Synonym
enalapril acid
BIDD:GT0752
AB00698268-08
AKOS015840130
mk-422
enalaprilat dihydrate
enalaprilic acid
MLS001424138
enalaprilat
enalaprilate
76420-72-9
1-((2s)-2-{[(1s)-1-carboxy-3-phenylpropyl]amino}propanoyl)-l-proline
EAL ,
enalaprilat inhibitor
smr000466359
MLS000759476
NCGC00164593-01
HMS2051H16
HMS2089P04
enalaprilat (anhydrous)
enalaprilatum
enalapril diacid
n-[(1s)-1-carboxy-3-phenylpropyl]-l-alanyl-l-proline
CHEBI:4786 ,
enalaprilat anhydrous
(2s)-1-[(2s)-2-[[(2s)-1-hydroxy-1-oxo-4-phenylbutan-2-yl]amino]propanoyl]pyrrolidine-2-carboxylic acid
(s)-1-((s)-2-(((s)-1-carboxy-3-phenylpropyl)amino)propanoyl)pyrrolidine-2-carboxylic acid
HMS3263O13
mk 422
l-proline, n-((1s)-1-carboxy-3-phenylpropyl)-l-alanyl-
q508q118jm ,
n-(1(s)-carboxy-3-phenylpropyl)-l-alanyl-l-proline
enalaprilate [french]
l-proline, 1-(n-(1-carboxt-3-phenylpropyl)-l-alanyl)-, (s)-
mk 421 diacid
enalaprilat [spanish]
einecs 278-459-3
enalaprilat [inn]
unii-q508q118jm
enalaprilatum [latin]
dtxsid0048975 ,
cas-76420-72-9
tox21_113430
dtxcid301265905
nsc760053
pharmakon1600-01503833
HMS2232B19
CCG-101042
bdbm50367254
LP01036
enalapril maleate impurity c [ep impurity]
1-(n-((s)-1-carboxy-3-phenylpropyl)-l-alanyl)-l-proline
enalapril diacid dihydrate anhydrous [mi]
(2s)-1-((2s)-2-(((1s)-1-carboxy-3-phenylpropyl)amino)propanoyl)pyrrolidine-2-carboxylic acid
l-proline, 1-(n-(1-carboxy-3-phenylpropyl)-l-alanyl)-, (s)-
AKOS015892570
gtpl6332
AB00698268-05
NC00292
SCHEMBL37289
NCGC00164593-02
tox21_113430_1
AB00698268-07
NCGC00261721-01
tox21_501036
W-104365
l-proline, n-[(1s)-1-carboxy-3-phenylpropyl]-l-alanyl-
AB00698268_09
AB00698268_10
mfcd00865786
(2s)-1-[(2s)-2-[[(1s)-1-carboxy-3-phenylpropyl]amino]propanoyl]pyrrolidine-2-carboxylic acid
sr-01000763426
SR-01000763426-3
enalaprilat, analytical standard
(2s)-1-[(2s)-2-{[(1s)-1-carboxy-3-phenylpropyl]amino}propanoyl]pyrrolidine-2-carboxylic acid
(2s)-1-[(2s)-2-[[(1s)-1-carboxy-3-phenylpropyl]amino]propanoyl]pyrrolidine-2-carboxylic acid (enalaprilat)
n-[(s)-1-carboxy-3-phenyl-propyl]-l-alanyl-l-proline
((s)-1-carboxy-3-phenylpropyl)-l-alanyl-l-proline
DB09477
(s)-1-((s)-2-((s)-1-carboxy-3-phenylpropylamino)propanoyl)pyrrolidine-2-carboxylic acid
Q5375179
enalaprilat,(s)
AS-13013
E1302
SDCCGSBI-0633781.P001
NCGC00164593-11
(s)-1-((s)-2-(((s)-1-carboxy-3-phenylpropyl)amino)propanoyl)pyrrolidine-2-carboxylicacid
EN300-123964
HY-B0231A
CS-0012359

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" However, little is known about the dosage-plasma-level relationship of ACE inhibitors in CHF and its relation to drug-induced adverse effects."( Plasma levels of enalaprilat in chronic therapy of heart failure: relationship to adverse events.
Brunner-La Rocca, HP; Follath, F; Kiowski, W; Maly, FE; Weilenmann, D, 1999
)
0.3
"Hypertensive emergency is a common problem requiring an effective, safe and easily administrable agent to reduce the blood pressure."( Evaluation of the efficacy, safety and tolerability of intravenous enalaprilat in the treatment of grade III essential hypertension in Indian patients.
Chembale, J; Kankane, A; Misra, M,
)
0.13

Pharmacokinetics

ExcerptReferenceRelevance
"The pharmacokinetic and pharmacodynamic profiles of oral enalapril (20 mg), in absence and in presence of probenecid pretreatment (1 g twice daily for 5 days), were investigated in 12 healthy volunteers on normal salt intake (150 mmol/24 hr)."( Pharmacokinetic and pharmacodynamic actions of enalapril in humans: effect of probenecid pretreatment.
Lant, AF; McNabb, WR; Noormohamed, FH, 1990
)
0.28
" The elimination half-life of enalaprilat was related to renal function."( The pharmacokinetics of enalapril in patients with compensated liver cirrhosis.
Baba, T; Murabayashi, S; Takebe, K; Tomiyama, T, 1990
)
0.28
" The pharmacokinetic differences observed are likely to be related to an age dependent decline in renal function as well as changes in body composition."( Age and the pharmacokinetics of angiotensin converting enzyme inhibitors enalapril and enalaprilat.
Ajayi, AA; Hockings, N; Reid, JL, 1986
)
0.27
"The effect of age on the pharmacodynamic responses to converting enzyme inhibitors, enalapril and enalaprilat was investigated in nine young (22-30 years) and nine sex-matched elderly (65-73 years), healthy volunteers."( Age and the pharmacodynamics of angiotensin converting enzyme inhibitors enalapril and enalaprilat.
Ajayi, AA; Hockings, N; Reid, JL, 1986
)
0.27
"The conventional pharmacokinetic profile of the angiotensin converting enzyme (ACE) inhibitor, enalapril, is a lipid-soluble and relatively inactive prodrug with good oral absorption (60 to 70%), a rapid peak plasma concentration (1 hour) and rapid clearance (undetectable by 4 hours) by de-esterification in the liver to a primary active diacid metabolite, enalaprilat."( Enalapril clinical pharmacokinetics and pharmacokinetic-pharmacodynamic relationships. An overview.
Elliott, HL; MacFadyen, RJ; Meredith, PA, 1993
)
0.29
"The pharmacokinetic parameters obtained for each formation were the area under the time-concentration curve from 0 to 24 h (AUC[0-24]), maximum concentration Cmax and the time at which it occurred (tmax)."( Bioequivalence study of two enalapril maleate tablet formulations in healthy male volunteers. Pharmacokinetic versus pharmacodynamic approach.
de Nucci, G; Martins, AR; Mendes, GB; Moreno, H; Muscará, MN; Ribeiro, W, 1996
)
0.29
"The results show that complete bioequivalence of the two formulations can be concluded from serum total enalapril concentration data, and that serum ACE activity is not a suitable pharmacodynamic variable for assessing bioequivalence."( Bioequivalence study of two enalapril maleate tablet formulations in healthy male volunteers. Pharmacokinetic versus pharmacodynamic approach.
de Nucci, G; Martins, AR; Mendes, GB; Moreno, H; Muscará, MN; Ribeiro, W, 1996
)
0.29
" Cmax and AUC values for enalaprilat in the maternal perfusate were approximately 3 times higher than in the fetal perfusate, and drug levels did not equilibrate between maternal and fetal perfusates during the 4-6 hours of perfusion."( Pharmacokinetic studies of enalaprilat in the in vitro perfused human placental lobule system.
Barrish, A; Gilbert, J; Jessee, L; Manson, JM; Miller, RK,
)
0.13
" Samples of blood were collected for determination of pharmacokinetic parameters."( Comparison of the pharmacokinetics of fosinoprilat with enalaprilat and lisinopril in patients with congestive heart failure and chronic renal insufficiency.
Caspi, A; Greenbaum, R; Liao, WC; Mangold, B; Nouriel, H; O'Grady, P; Paz, R; Sclarovsky, S; Yee, KF; Zucchelli, P, 2000
)
0.31
" The median effective half-life for accumulation ranged from 14."( The pharmacokinetics of enalapril in children and infants with hypertension.
Blowey, D; Delucchi, A; Hand, E; Hogg, R; Lo, MW; Panebianco, D; Rippley, R; Sakarcan, A; Shahinfar, S; Shaw, W; Vogt, B; Walson, P; Wells, T, 2001
)
0.31
" These plasma concentrations and blood pressure measurements were applied to evaluate the pharmacokinetic (PK) and pharmacodynamic (PD) parameters of both enalapril and enalaprilat."( Determination of enalapril and enalaprilat by enzyme linked immunosorbent assays: application to pharmacokinetic and pharmacodynamic analysis.
Arafat, T; Hamad, M; Jehanli, A; Matalka, K, 2002
)
0.31
"5 mg/kg PO did not demonstrate significant availability, pharmacodynamic effect, or substantial suppression of ACE activity."( Characterization of the pharmacokinetic and pharmacodynamic properties of the angiotensin-converting enzyme inhibitor, enalapril, in horses.
Atkins, CE; Gardner, SY; Papich, MG; Sams, RA; Schwabenton, AB,
)
0.13
"Most of the pharmacokinetic (PK) parameters for enalapril and enalaprilat were established following determination of the drug and its metabolite, using angiotensin converting enzyme (ACE) inhibition assays."( Pharmacokinetics and pharmacodynamics profiles of enalapril maleate in healthy volunteers following determination of enalapril and enalaprilat by two specific enzyme immunoassays.
Al-Nasan, A; Arafat, T; Awad, R; Azzam, R; Hamad, M; Jehanli, A; Matalka, K, 2005
)
0.33
"6 ng h/mL, Cmax values were 313."( Pharmacokinetics and pharmacodynamics profiles of enalapril maleate in healthy volunteers following determination of enalapril and enalaprilat by two specific enzyme immunoassays.
Al-Nasan, A; Arafat, T; Awad, R; Azzam, R; Hamad, M; Jehanli, A; Matalka, K, 2005
)
0.33
" pharmacokinetic data on 670 drugs representing, to our knowledge, the largest publicly available set of human clinical pharmacokinetic data."( Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
Lombardo, F; Obach, RS; Waters, NJ, 2008
)
0.35
" The HPLC-MS/MS method herein described was fully validated and successfully applied to the pharmacokinetic study of enalapril maleate capsules in 20 healthy male volunteers after oral administration."( Simultaneous quantification of enalapril and enalaprilat in human plasma by high-performance liquid chromatography-tandem mass spectrometry and its application in a pharmacokinetic study.
Jiang, K; Li, F; Lu, S; Lu, X; Qin, F, 2009
)
0.35
" The method described herein was fully validated and successfully applied to the pharmacokinetic study of lisinopril tablets in healthy male volunteers after oral administration."( Quantitative determination of lisinopril in human plasma by high performance liquid chromatography-tandem mass spectrometry and its application in a pharmacokinetic study.
Jing, L; Li, F; Qin, F; Wang, D; Xiong, Z; Yang, S, 2012
)
0.38
"Compared with control group and nephrotic group received enalapril alone respectively, Tmax of enalaprilat in nephrotic group received both enalapril and candesartan cilexetil prolonged about 21."( The effect of candesartan on the pharmacokinetics of enalaprilat in nephrotic rats.
Bi, BT; Lin, HB; Lin, T; Ma, AD; Xu, JP; Yang, XM; Yang, YB, 2012
)
0.38
" The CES1 genotype had no significant effect on the enalaprilat to enalapril AUC0-∞ ratio or on any other pharmacokinetic or pharmacodynamic parameters of enalapril or enalaprilat."( Effect of carboxylesterase 1 c.428G > A single nucleotide variation on the pharmacokinetics of quinapril and enalapril.
Backman, JT; Holmberg, MT; Launiainen, T; Neuvonen, PJ; Niemi, M; Tarkiainen, EK; Tornio, A, 2015
)
0.42

Compound-Compound Interactions

ExcerptReferenceRelevance
" Although the participation of the particular transporters in observed drug-drug interactions can be difficult to confirm in humans, this review focuses mainly on pharmacokinetic interactions of clinically important drugs."( Transporter-mediated Drug Interactions.
Tsuji, A, 2002
)
0.31

Bioavailability

ExcerptReferenceRelevance
" Parent drug absorption and diacid bioavailability in the rat were higher than for enalapril, and the inhibition of plasma ACE of longer duration."( Biological properties of the angiotensin-converting enzyme inhibitor cilazapril.
Brewster, M; Budd, J; Francis, RJ; Klevans, LR; Natoff, IL; Nixon, JS; Patel, AT; Wenger, J; Worth, E,
)
0.13
" This study did not take bioavailability into consideration."( Visual compatibility of enalaprilat with commonly used critical care medications during simulated Y-site injection.
Alicea, M; Colucci, RD; Greenstein, R; Halpern, NA, 1989
)
0.28
" Enalapril is a prodrug that is well absorbed from the gastrointestinal tract, with 60 to 70% of an oral dose being absorbed."( Clinical pharmacokinetics of the angiotensin converting enzyme inhibitors. A review.
Cody, RJ; Kubo, SH,
)
0.13
" Drug disposition studies in rats, dogs, and monkeys have demonstrated that the method can be readily adapted to any ACE inhibitor and is suitable for determining drug bioavailability and pharmacokinetics."( Radioenzymatic assay of angiotensin-converting enzyme inhibitors in plasma and urine.
Alpaugh, WC; Stauber, KL; Swanson, BN; Weinstein, SH, 1985
)
0.27
" In rats, but not in dogs, the diacid inhibitor was poorly absorbed, whereas MK-421 was well absorbed in both species."( Effect of N-[(S)-1-carboxy-3-phenylpropyl]-L-Ala-L-Pro and its ethyl ester (MK-421) on angiotensin converting enzyme in vitro and angiotensin I pressor responses in vivo.
Backlund, EP; Bohn, DL; Gross, DM; Morris, AA; Stone, CA; Sweet, CS; Ulm, EH; Vassil, TC; Weitz, D; Wenger, HC, 1981
)
0.26
"Two different conventional release enalapril maleate tablet formulations were evaluated for their relative bioavailability (Eupressin tablets 10 mg, Biosintética as the test formulation vs Renitec tablets 10 mg Merck Sharp & Dhome, as the reference formulation)."( Bioequivalence study of two enalapril maleate tablet formulations in healthy male volunteers. Pharmacokinetic versus pharmacodynamic approach.
de Nucci, G; Martins, AR; Mendes, GB; Moreno, H; Muscará, MN; Ribeiro, W, 1996
)
0.29
" However, no difference in either the extent or the rate of absorption were observed when serum total enalapril vs time curves were analysed."( Bioequivalence study of two enalapril maleate tablet formulations in healthy male volunteers. Pharmacokinetic versus pharmacodynamic approach.
de Nucci, G; Martins, AR; Mendes, GB; Moreno, H; Muscará, MN; Ribeiro, W, 1996
)
0.29
"Enalaprilat is a typical angiotensin-converting enzyme inhibitor and is very poorly absorbed from the gastrointestinal tract."( Investigation of polymeric nanoparticles as carriers of enalaprilat for oral administration.
Ahlin, P; Kristl, A; Kristl, J; Vrecer, F, 2002
)
0.31
"To compare the relative bioavailability and bioequivalence of 2 enalapril tablet formulations in healthy volunteers under fasting conditions."( Bioequivalence study of two brands of enalapril tablets after single oral administration to healthy volunteers.
Daftsios, AC; Nikolaidis, N; Niopas, I, 2003
)
0.32
"From the results of the present study, it is concluded that the test and reference tablet formulations of enalapril are bioequivalent for both the extent and the rate of absorption and therefore the 2 products can be considered to be interchangeable in clinical practice."( Bioequivalence study of two brands of enalapril tablets after single oral administration to healthy volunteers.
Daftsios, AC; Nikolaidis, N; Niopas, I, 2003
)
0.32
"The pharmacokinetic and relative bioavailability studies of 20-mg enalapril tablets, the test product manufactured by Biolab, Thailand compared to the reference product (Merck Sharp & Dohme, USA) was conducted in 14 healthy Thai male volunteers following a single dose, two-period, crossover design."( Relative bioavailability study of 20-mg enalapril tablets in healthy male volunteers.
Lohitnavy, M; Lohitnavy, O; Polnok, S; Taytiwat, P, 2003
)
0.32
"05), whereas the response to an NO donor was unaffected, suggesting decreased bioavailability of NO."( Oxidant stress leads to impaired regulation of renal cortical oxygen consumption by nitric oxide in the aging kidney.
Adler, S; Huang, H; Kaminski, PM; Wolin, MS, 2004
)
0.32
" Thus NO bioavailability is impaired in SHR owing to an ANG II-mediated increase in superoxide production in association with enhanced expression of NAD(P)H oxidase components, despite increased expression of eNOS."( Oxidant stress in kidneys of spontaneously hypertensive rats involves both oxidase overexpression and loss of extracellular superoxide dismutase.
Adler, S; Huang, H, 2004
)
0.32
"Angiotensin-converting enzyme (ACE) inhibitors increase the bioavailability of bradykinin, which induces cardiac PC."( Pretreatment with intracoronary enalaprilat protects human myocardium during percutaneous coronary angioplasty.
Bolli, R; Jneid, H; Leesar, MA; Tang, XL, 2007
)
0.34
" This response is endothelium mediated and involves the reduction of NO bioavailability and the action of reactive oxygen species."( Low nanomolar concentration of mercury chloride increases vascular reactivity to phenylephrine and local angiotensin production in rats.
Oliveira, EM; Padilha, AS; Peçanha, FM; Stefanon, I; Vassallo, DV; Wiggers, GA, 2008
)
0.35
"Oral bioavailability (F) is a product of fraction absorbed (Fa), fraction escaping gut-wall elimination (Fg), and fraction escaping hepatic elimination (Fh)."( Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
Chang, G; El-Kattan, A; Miller, HR; Obach, RS; Rotter, C; Steyn, SJ; Troutman, MD; Varma, MV, 2010
)
0.36
" Moreover, the increased reactivity to PHE promoted by Gd was endothelium-dependent, reducing NO bioavailability and involving an increased stimulation of angiotensin-converting enzyme and angiotensin II AT1 receptors."( Gadolinium increases the vascular reactivity of rat aortic rings.
Angeli, JK; Casali, EA; Fürstenau, CR; Ramos, DB; Sarkis, JJ; Souza, DO; Stefanon, I; Vassallo, DV, 2011
)
0.37
"The development of oral modified-release (MR) dosage forms requires an active pharmaceutical ingredient (API) with a sufficiently high absorption rate in both the small and large intestine."( Regional Intestinal Permeability in Dogs: Biopharmaceutical Aspects for Development of Oral Modified-Release Dosage Forms.
Abrahamsson, B; Dahlgren, D; Johansson, P; Lennernäs, H; Lundqvist, A; Roos, C; Sjögren, E; Tannergren, C, 2016
)
0.43
"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
" We hypothesize that sGC stimulator Compound 1 can enhance NO signaling, reduce proteinuria in a diabetic nephropathy preclinical model with diminished NO bioavailability and increased oxidized sGC."( Effects of soluble guanylate cyclase stimulator on renal function in ZSF-1 model of diabetic nephropathy.
Blumenschein, W; Chen, Y; Cox, J; Grein, J; Hoek, M; Hu, L; Lin, K; Liu, Y; Swaminath, G; Zhou, X,
)
0.13
"Nanocarriers provide a number of undeniable advantages that could improve the bioavailability of active agents for human, animal, and plant cells."( A Direct Comparison of Peptide Drug Delivery Systems Based on the Use of Hybrid Calcium Phosphate/Chitosan Nanoparticles versus Unmixed Calcium Phosphate or Chitosan Nanoparticles In Vitro and In Vivo.
Beznos, O; Chesnokova, N; Grigoriev, Y; Kost, O; Popova, E; Taliansky, M; Tikhomirova, V, 2023
)
0.91

Dosage Studied

ExcerptRelevanceReference
"In previously untreated rats, pretreatment with enalaprilat shifted the dose-response curve for the hypotensive effect of doxazosin to the left, indicating synergism."( A study of the interaction between the hypotensive actions of doxazosin and enalaprilat in anaesthetized rats.
Marwood, JF; Stokes, GS; Tierney, G, 1992
)
0.28
" On repeated daily oral dosing to SHR, both compounds had a cumulative antihypertensive effect."( Biological properties of the angiotensin-converting enzyme inhibitor cilazapril.
Brewster, M; Budd, J; Francis, RJ; Klevans, LR; Natoff, IL; Nixon, JS; Patel, AT; Wenger, J; Worth, E,
)
0.13
" Twenty and 40 mg enalapril lowered the blood pressure by 2 h after dosing in the hypertension group, and peak effects were seen 4-5 h after dosing."( Pharmacokinetics and pharmacodynamics of enalapril in patients with congestive heart failure and patients with hypertension.
Abernethy, D; Farmer, J; Mitchell, JR; Nelson, E; O'Meara, M; Pool, J; Schwartz, JB; Taylor, A; Young, J,
)
0.13
" A conversion rate of angiotensin I to angiotensin II calculated from the dose-response curves was 26."( Presynaptic angiotensin II receptors and captopril-induced adrenergic transmission failure probably not via converting enzyme inhibition in guinea-pig pulmonary arteries.
Kubo, T; Misu, Y; Shionoiri, H; Yasuda, G, 1987
)
0.27
" The design of dosage regimens of both lisinopril and enalapril for patients with severe renal impairment or chronic renal failure should take into consideration the use and effects of haemodialysis."( Pharmacokinetics of lisinopril, enalapril and enalaprilat in renal failure: effects of haemodialysis.
Carmody, M; Cooper, WD; Doyle, GD; Glover, DR; Kelly, JG, 1988
)
0.27
" Further study of the usefulness of chronic dosing with angiotensin converting enzyme inhibitors in hypertension in the elderly is indicated."( Age and the pharmacodynamics of angiotensin converting enzyme inhibitors enalapril and enalaprilat.
Ajayi, AA; Hockings, N; Reid, JL, 1986
)
0.27
" Both acutely and chronically in patients with essential hypertension, enalapril reduced blood pressure with a rather flat dose-response curve."( An overview of the clinical pharmacology of enalapril.
Davies, RO; Gomez, HJ; Irvin, JD; Walker, JF, 1984
)
0.27
" During long-term administration of enalapril, a similar relationship between the plasma enalaprilic acid level, ACE inhibition and the hypotensive effect was shown, although the dose-response curve for plasma enalaprilic acid to ACE inhibition was displaced to the right compared to the acute dose-response curve."( Plasma enalapril levels and hormonal effects after short- and long-term administration in essential hypertension.
Casley, D; Cubella, R; Jackson, BJ; Johnston, CI; Larmour, I, 1984
)
0.27
" However, when compared to the acute response, the ACE inhibition dose-response line was shifted to the right after chronic enalapril therapy suggesting that enalapril may lead to ACE induction in humans."( Relationship of antihypertensive effect of enalapril to serum MK-422 levels and angiotensin converting enzyme inhibition.
Arnolda, L; Jackson, B; Johnston, CI; Matthews, G; McGrath, B, 1983
)
0.27
" Serum profiles after chronic dosing of enalapril show little accumulation of the active diacid metabolite, enalaprilat."( Kinetic and metabolic aspects of enalapril action.
Lant, AF; McNabb, RW; Noormohamed, FH, 1984
)
0.27
" During repeated dosing in the outpatient trial there was attenuation of the antihypertensive effect (12 to 24 hr after dosing) in eight of 10 patients."( Effects of enalapril, a new converting enzyme inhibitor, in hypertension.
Ferguson, RK; Hichens, M; Huber, PB; Irvin, JD; Mojaverian, P; Swanson, BN; Vlasses, PH, 1982
)
0.26
"We investigated the dose-dependent cardiovascular effects of enalaprilat at different dosing times in two animal models of hypertension."( Effects of enalaprilat on circadian profiles in blood pressure and heart rate of spontaneously and transgenic hypertensive rats.
Ganten, D; Lemmer, B; Makabe, T; Mattes, A; Witte, K, 1994
)
0.29
"Intracoronary enalaprilat at a dosage that did not cause systemic neurohormonal activation improved LV diastolic chamber distensibility and regional relaxation and filling in patients with LV hypertrophy due to aortic stenosis."( Intracardiac angiotensin-converting enzyme inhibition improves diastolic function in patients with left ventricular hypertrophy due to aortic stenosis.
Benedict, C; Douglas, PS; Friedrich, SP; Gordon, S; Hayashida, W; Hess, OM; Keighley, CS; Krayenbuehl, HP; Lorell, BH; Rousseau, MF, 1994
)
0.29
" In contrast, combined treatment with enalapril and AVPA resulted in a 36 +/- 11% decrease in blood pressure after epidural dosing (n = 6)."( Endogenous vasopressin and renin-angiotensin systems support blood pressure after epidural block in humans.
Carp, H; Garvey, D; Jayaram, A; Vadhera, R, 1994
)
0.29
" The oral dosage should be much reduced in infants with congestive heart failure aged < 20 days compared with those aged > 20 days."( The kinetic profiles of enalapril and enalaprilat and their possible developmental changes in pediatric patients with congestive heart failure.
Chiba, K; Ishii, M; Ishizaki, T; Kato, H; Nakamura, H; Sugimura, T, 1994
)
0.29
" The inhibition of ACE activity paralleled enalaprilat concentrations following both single and multiple dosing and the time of maximum inhibition of ACE activity was associated on both occasions with maximum concentration of enalaprilat."( Enalapril pharmacokinetics and ACE inhibition, following single and chronic oral dosing.
Edeki, T; Johnston, A; Li Kam Wa, E; Turner, P, 1994
)
0.29
"2 L/h)] results in significant accumulation of enalaprilat and necessitates dosage reduction."( Enalapril clinical pharmacokinetics and pharmacokinetic-pharmacodynamic relationships. An overview.
Elliott, HL; MacFadyen, RJ; Meredith, PA, 1993
)
0.29
" Neither afferent nor efferent arteriolar Ang II dose-response relations were significantly different in kidneys treated with low-dose adenosine or the adenosine receptor blocker."( Renal arteriolar angiotensin responses during varied adenosine receptor activation.
Carmines, PK; Inscho, EW, 1994
)
0.29
" We found that saralasin or DuP 753, but not the kinin antagonist, displaced the dose-response curve to the right."( Oxytocic effect of trypsin on the isolated rat uterus.
Castillo, G; Esteban, S; Orce, G, 1994
)
0.29
" Oral dosing with active drugs led to different temporal responses."( Blood pressure response to the first dose of angiotensin-converting enzyme inhibitors in congestive heart failure.
Lees, KR; MacFadyen, RJ; Reid, JL; Squire, IB, 1993
)
0.29
" Subchronic dosing at 7 PM significantly further decreased nighttime blood pressure followed by a slow increase during the day, with no effect on elevated afternoon values."( Cardiovascular effects, pharmacokinetics, and converting enzyme inhibition of enalapril after morning versus evening administration.
Hopf, R; Lehmann, K; Lemmer, B; Mutschler, E; Neubeck, M; Weisser, K; Witte, K, 1993
)
0.29
" Enalaprilat levels were measured and compared with 15 similar patients matched for transplant function and enalapril dosage immunosuppressed with cyclosporine and prednisone."( Mechanism of angiotensin converting enzyme inhibitor-related anemia in renal transplant recipients.
Bachmann, T; Gossmann, J; Kachel, HG; Scheuermann, EH; Schoeppe, W; Thürmann, P; Weller, S, 1996
)
0.29
"1 mumol/L) had no alpha 1-adrenoceptor antagonist effect but altered the mode of action of the alpha 1-adrenoceptor antagonist doxazosin: PD123319 changed doxazosin from a competitive to a non-competitive antagonist, as evidenced by the reduced slope of the dose-response curve for the alpha 1-adrenoceptor agonist phenylephrine."( Effect of angiotensin II receptor blockade on the interaction between enalaprilat and doxazosin in rat tail arteries.
Marwood, JF,
)
0.13
" Dose-response curves were constructed before and during enalaprilat coinfusion (1 microg/min for 40 minutes)."( Angiotensin-converting enzyme inhibition improves venous endothelial dysfunction in chronic smokers.
Blaschke, TF; Chalon, S; Hoffman, BB; Moreno, H, 1999
)
0.3
" ACE inhibition shifted the bradykinin dose-response curve to the left in both groups (P < ."( Angiotensin-converting enzyme inhibition improves venous endothelial dysfunction in chronic smokers.
Blaschke, TF; Chalon, S; Hoffman, BB; Moreno, H, 1999
)
0.3
"We investigated 45 patients (age 55 +/- 10 years) with stable CHF who presented with a maintenance dosage of enalapril of either 5 mg given twice daily (E10; n = 16), 10 mg given twice daily (E20; n = 18), or 20 mg given twice daily (E40; n = 11)."( Within-patient comparison of effects of different dosages of enalapril on functional capacity and neurohormone levels in patients with chronic heart failure.
Brunner-La Rocca, HP; Candinas, R; Follath, F; Kiowski, W; Maly, FE; Weilenmann, D, 1999
)
0.3
" Thus patients with congestive heart failure may benefit from increasing dosage of ACE inhibitors."( Within-patient comparison of effects of different dosages of enalapril on functional capacity and neurohormone levels in patients with chronic heart failure.
Brunner-La Rocca, HP; Candinas, R; Follath, F; Kiowski, W; Maly, FE; Weilenmann, D, 1999
)
0.3
" At the lowest dose studied (20 microgram/kg iv), the inhibitory effects of candesartan were competitive, whereas at the highest dose (100 microgram/kg iv) the dose-response curve for angiotensin II was shifted to the right in a nonparallel manner with inhibitory effects that could not be surmounted."( Role of AT(1) receptors and autonomic nervous system in mediating acute pressor responses to ANG II in anesthetized mice.
Bivalacqua, TJ; Champion, HC; Dalal, A; Kadowitz, PJ, 1999
)
0.3
"To compare the serum pharmacokinetics of fosinoprilat with enalaprilat and lisinopril after 1 and 10 days of dosing with fosinopril, enalapril and lisinopril."( Comparison of the pharmacokinetics of fosinoprilat with enalaprilat and lisinopril in patients with congestive heart failure and chronic renal insufficiency.
Caspi, A; Greenbaum, R; Liao, WC; Mangold, B; Nouriel, H; O'Grady, P; Paz, R; Sclarovsky, S; Yee, KF; Zucchelli, P, 2000
)
0.31
"Angiotensin I-converting enzyme (ACE/kininase II) inhibitors potentiated guinea pig ileum's isotonic contractions to bradykinin (BK) and its analogues, shifting the BK dose-response curve to the left."( Potentiation of the effects of bradykinin on its receptor in the isolated guinea pig ileum.
Erdös, EG; Igić, R; Minshall, RD; Nedumgottil, SJ; Rabito, SF, 2000
)
0.31
" We studied whether the dosage of enalapril in daily clinical practice is associated with drug accumulation of enalaprilat in chronic renal failure."( High serum enalaprilat in chronic renal failure.
Elung-Jensen, T; Heisterberg, J; Kamper, AL; Larsen, NE; Sonne, J; Strandgaard, S, 2001
)
0.31
"Enalaprilat shifted the norepinephrine dose-response curve to the right (P=0."( Effects of enalaprilat on venoconstriction to norepinephrine: role of prostaglandins.
Arnold, JM; Dzeka, TN; Townley, R, 2003
)
0.32
" In dose-finding experiments in non-hypertrophied isolated perfused hearts, we performed dose-response curves of losartan and enalaprilat studying monophasic action potential duration at 90% repolarisation (MAPD(90%)) and ventricular fibrillation (VF) threshold."( Losartan but not enalaprilat acutely reduces reperfusion ventricular tachyarrhythmias in hypertrophied rat hearts after low-flow ischaemia.
Beier, K; Bellahcene, M; Buser, PT; Butz, S; Driamov, S; Remondino, A; Zaugg, CE; Ziegler, A, 2004
)
0.32
" Since marked inter-patient variation in concentrations of enalaprilat has been shown in patients with renal failure despite equivalent dosage of enalapril, a direct comparison of the effect of high versus low plasma concentrations of enalaprilat on the progression of renal failure was undertaken."( Enalapril dosage in progressive chronic nephropathy: a randomised, controlled trial.
Elung-Jensen, T; Heisterberg, J; Kamper, AL; Sonne, J; Strandgaard, S, 2005
)
0.33
" Pharmacokinetic data are lacking to provide adequate dosing and for pediatric pharmacotherapeutical trials it is imperative to minimize sample volume."( Determination of enalapril and enalaprilat in small human serum quantities for pediatric trials by HPLC-tandem mass spectrometry.
Läer, S; Ramusovic, S; Thielking, G, 2012
)
0.38
" In view of these findings, we should lower dosage and prolong dosing interval for nephrotic patients in the combination of enalapril and candesartan."( The effect of candesartan on the pharmacokinetics of enalaprilat in nephrotic rats.
Bi, BT; Lin, HB; Lin, T; Ma, AD; Xu, JP; Yang, XM; Yang, YB, 2012
)
0.38
" The findings suggest that appropriately dosed ACE-I with or without steroids may be a new therapeutic agent for colitis."( Angiotensin converting enzyme-inhibitor reduces colitis severity in an IL-10 knockout model.
Daignault, S; Ignatoski, KM; Okawada, M; Sueyoshi, R; Teitelbaum, DH, 2013
)
0.39
"The development of oral modified-release (MR) dosage forms requires an active pharmaceutical ingredient (API) with a sufficiently high absorption rate in both the small and large intestine."( Regional Intestinal Permeability in Dogs: Biopharmaceutical Aspects for Development of Oral Modified-Release Dosage Forms.
Abrahamsson, B; Dahlgren, D; Johansson, P; Lennernäs, H; Lundqvist, A; Roos, C; Sjögren, E; Tannergren, C, 2016
)
0.43
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (2)

RoleDescription
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).
antihypertensive agentAny drug used in the treatment of acute or chronic vascular hypertension regardless of pharmacological mechanism.
[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 (2)

ClassDescription
dicarboxylic acidAny carboxylic acid containing two carboxy groups.
dipeptideAny molecule that contains two amino-acid residues connected by peptide linkages.
[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 (14)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency5.95570.001530.607315,848.9004AID1224848; AID1224849
estrogen nuclear receptor alphaHomo sapiens (human)Potency26.83250.000229.305416,493.5996AID743069
[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)
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50 (µMol)133.00000.63154.45319.3000AID1473740
Multidrug resistance-associated protein 4Homo sapiens (human)IC50 (µMol)133.00000.20005.677410.0000AID1473741
Bile salt export pumpHomo sapiens (human)IC50 (µMol)566.50000.11007.190310.0000AID1449628; AID1473738
Angiotensin-converting enzymeMus musculus (house mouse)IC50 (µMol)0.01150.01150.01150.0115AID1466506
Angiotensin-converting enzyme Homo sapiens (human)IC50 (µMol)0.24050.00010.533610.0000AID1466507; AID37639; AID38849; AID38852; AID38853; AID38859; AID38864; AID39616; AID39622; AID39750; AID39758
Angiotensin-converting enzymeOryctolagus cuniculus (rabbit)IC50 (µMol)0.00540.00001.612910.0000AID37656; AID37658; AID37671; AID37930
Angiotensin-converting enzymeOryctolagus cuniculus (rabbit)Ki0.00140.00042.03378.6606AID37801
Dipeptidyl peptidase 4Homo sapiens (human)IC50 (µMol)100.00000.00010.444410.0000AID1466504
Type-2 angiotensin II receptorRattus norvegicus (Norway rat)IC50 (µMol)0.00120.00100.39573.3000AID39622
Angiotensin-converting enzymeRattus norvegicus (Norway rat)IC50 (µMol)0.00360.00090.33223.0300AID1466505; AID37962; AID38086; AID38089; AID39616
Angiotensin-converting enzyme 2Rattus norvegicus (Norway rat)Ki0.00050.00050.00050.0005AID38847
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50 (µMol)133.00002.41006.343310.0000AID1473739
Angiotensin-converting enzyme 2 Homo sapiens (human)IC50 (µMol)0.00240.00042.207910.0000AID39758
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (132)

Processvia Protein(s)Taxonomy
xenobiotic metabolic processATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
bile acid and bile salt transportATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transportATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
leukotriene transportATP-binding cassette sub-family C member 3Homo sapiens (human)
monoatomic anion transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transport across blood-brain barrierATP-binding cassette sub-family C member 3Homo sapiens (human)
prostaglandin secretionMultidrug resistance-associated protein 4Homo sapiens (human)
cilium assemblyMultidrug resistance-associated protein 4Homo sapiens (human)
platelet degranulationMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic metabolic processMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
bile acid and bile salt transportMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transportMultidrug resistance-associated protein 4Homo sapiens (human)
urate transportMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
cAMP transportMultidrug resistance-associated protein 4Homo sapiens (human)
leukotriene transportMultidrug resistance-associated protein 4Homo sapiens (human)
monoatomic anion transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
export across plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
transport across blood-brain barrierMultidrug resistance-associated protein 4Homo sapiens (human)
guanine nucleotide transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo sapiens (human)
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)
behavioral fear responseDipeptidyl peptidase 4Homo sapiens (human)
response to hypoxiaDipeptidyl peptidase 4Homo sapiens (human)
proteolysisDipeptidyl peptidase 4Homo sapiens (human)
cell adhesionDipeptidyl peptidase 4Homo sapiens (human)
positive regulation of cell population proliferationDipeptidyl peptidase 4Homo sapiens (human)
negative regulation of extracellular matrix disassemblyDipeptidyl peptidase 4Homo sapiens (human)
peptide hormone processingDipeptidyl peptidase 4Homo sapiens (human)
receptor-mediated endocytosis of virus by host cellDipeptidyl peptidase 4Homo sapiens (human)
T cell costimulationDipeptidyl peptidase 4Homo sapiens (human)
regulation of cell-cell adhesion mediated by integrinDipeptidyl peptidase 4Homo sapiens (human)
locomotory exploration behaviorDipeptidyl peptidase 4Homo sapiens (human)
psychomotor behaviorDipeptidyl peptidase 4Homo sapiens (human)
T cell activationDipeptidyl peptidase 4Homo sapiens (human)
endothelial cell migrationDipeptidyl peptidase 4Homo sapiens (human)
symbiont entry into host cellDipeptidyl peptidase 4Homo sapiens (human)
receptor-mediated virion attachment to host cellDipeptidyl peptidase 4Homo sapiens (human)
negative chemotaxisDipeptidyl peptidase 4Homo sapiens (human)
membrane fusionDipeptidyl peptidase 4Homo sapiens (human)
negative regulation of neutrophil chemotaxisDipeptidyl peptidase 4Homo sapiens (human)
glucagon processingDipeptidyl peptidase 4Homo sapiens (human)
xenobiotic metabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
negative regulation of gene expressionCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bile acid and bile salt transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
heme catabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic export from cellCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transepithelial transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
leukotriene transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
monoatomic anion transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
negative regulation of signaling receptor activityAngiotensin-converting enzyme 2 Homo sapiens (human)
symbiont entry into host cellAngiotensin-converting enzyme 2 Homo sapiens (human)
regulation of cytokine productionAngiotensin-converting enzyme 2 Homo sapiens (human)
angiotensin maturationAngiotensin-converting enzyme 2 Homo sapiens (human)
angiotensin-mediated drinking behaviorAngiotensin-converting enzyme 2 Homo sapiens (human)
regulation of systemic arterial blood pressure by renin-angiotensinAngiotensin-converting enzyme 2 Homo sapiens (human)
tryptophan transportAngiotensin-converting enzyme 2 Homo sapiens (human)
viral life cycleAngiotensin-converting enzyme 2 Homo sapiens (human)
receptor-mediated endocytosis of virus by host cellAngiotensin-converting enzyme 2 Homo sapiens (human)
regulation of vasoconstrictionAngiotensin-converting enzyme 2 Homo sapiens (human)
regulation of transmembrane transporter activityAngiotensin-converting enzyme 2 Homo sapiens (human)
regulation of cell population proliferationAngiotensin-converting enzyme 2 Homo sapiens (human)
symbiont entry into host cellAngiotensin-converting enzyme 2 Homo sapiens (human)
receptor-mediated virion attachment to host cellAngiotensin-converting enzyme 2 Homo sapiens (human)
negative regulation of smooth muscle cell proliferationAngiotensin-converting enzyme 2 Homo sapiens (human)
regulation of inflammatory responseAngiotensin-converting enzyme 2 Homo sapiens (human)
positive regulation of amino acid transportAngiotensin-converting enzyme 2 Homo sapiens (human)
maternal process involved in female pregnancyAngiotensin-converting enzyme 2 Homo sapiens (human)
positive regulation of cardiac muscle contractionAngiotensin-converting enzyme 2 Homo sapiens (human)
membrane fusionAngiotensin-converting enzyme 2 Homo sapiens (human)
negative regulation of ERK1 and ERK2 cascadeAngiotensin-converting enzyme 2 Homo sapiens (human)
blood vessel diameter maintenanceAngiotensin-converting enzyme 2 Homo sapiens (human)
entry receptor-mediated virion attachment to host cellAngiotensin-converting enzyme 2 Homo sapiens (human)
positive regulation of gap junction assemblyAngiotensin-converting enzyme 2 Homo sapiens (human)
regulation of cardiac conductionAngiotensin-converting enzyme 2 Homo sapiens (human)
positive regulation of L-proline import across plasma membraneAngiotensin-converting enzyme 2 Homo sapiens (human)
positive regulation of reactive oxygen species metabolic processAngiotensin-converting enzyme 2 Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (51)

Processvia Protein(s)Taxonomy
ATP bindingATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type xenobiotic transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type bile acid transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATP hydrolysis activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
icosanoid transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
guanine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ATP bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type xenobiotic transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
urate transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
purine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type bile acid transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
efflux transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
15-hydroxyprostaglandin dehydrogenase (NAD+) activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATP hydrolysis activityMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo sapiens (human)
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)
virus receptor activityDipeptidyl peptidase 4Homo sapiens (human)
protease bindingDipeptidyl peptidase 4Homo sapiens (human)
aminopeptidase activityDipeptidyl peptidase 4Homo sapiens (human)
serine-type endopeptidase activityDipeptidyl peptidase 4Homo sapiens (human)
signaling receptor bindingDipeptidyl peptidase 4Homo sapiens (human)
protein bindingDipeptidyl peptidase 4Homo sapiens (human)
serine-type peptidase activityDipeptidyl peptidase 4Homo sapiens (human)
dipeptidyl-peptidase activityDipeptidyl peptidase 4Homo sapiens (human)
identical protein bindingDipeptidyl peptidase 4Homo sapiens (human)
protein homodimerization activityDipeptidyl peptidase 4Homo sapiens (human)
chemorepellent activityDipeptidyl peptidase 4Homo sapiens (human)
protein bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
organic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type xenobiotic transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP hydrolysis activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
virus receptor activityAngiotensin-converting enzyme 2 Homo sapiens (human)
endopeptidase activityAngiotensin-converting enzyme 2 Homo sapiens (human)
carboxypeptidase activityAngiotensin-converting enzyme 2 Homo sapiens (human)
metallocarboxypeptidase activityAngiotensin-converting enzyme 2 Homo sapiens (human)
protein bindingAngiotensin-converting enzyme 2 Homo sapiens (human)
metallopeptidase activityAngiotensin-converting enzyme 2 Homo sapiens (human)
peptidyl-dipeptidase activityAngiotensin-converting enzyme 2 Homo sapiens (human)
zinc ion bindingAngiotensin-converting enzyme 2 Homo sapiens (human)
identical protein bindingAngiotensin-converting enzyme 2 Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (32)

Processvia Protein(s)Taxonomy
plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basal plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basolateral plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
nucleolusMultidrug resistance-associated protein 4Homo sapiens (human)
Golgi apparatusMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
platelet dense granule membraneMultidrug resistance-associated protein 4Homo sapiens (human)
external side of apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
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)
extracellular regionDipeptidyl peptidase 4Homo sapiens (human)
lysosomal membraneDipeptidyl peptidase 4Homo sapiens (human)
plasma membraneDipeptidyl peptidase 4Homo sapiens (human)
focal adhesionDipeptidyl peptidase 4Homo sapiens (human)
cell surfaceDipeptidyl peptidase 4Homo sapiens (human)
membraneDipeptidyl peptidase 4Homo sapiens (human)
apical plasma membraneDipeptidyl peptidase 4Homo sapiens (human)
lamellipodiumDipeptidyl peptidase 4Homo sapiens (human)
endocytic vesicleDipeptidyl peptidase 4Homo sapiens (human)
lamellipodium membraneDipeptidyl peptidase 4Homo sapiens (human)
membrane raftDipeptidyl peptidase 4Homo sapiens (human)
intercellular canaliculusDipeptidyl peptidase 4Homo sapiens (human)
extracellular exosomeDipeptidyl peptidase 4Homo sapiens (human)
plasma membraneDipeptidyl peptidase 4Homo sapiens (human)
plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
cell surfaceCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
intercellular canaliculusCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
plasma membraneAngiotensin-converting enzyme 2 Homo sapiens (human)
extracellular regionAngiotensin-converting enzyme 2 Homo sapiens (human)
extracellular spaceAngiotensin-converting enzyme 2 Homo sapiens (human)
endoplasmic reticulum lumenAngiotensin-converting enzyme 2 Homo sapiens (human)
plasma membraneAngiotensin-converting enzyme 2 Homo sapiens (human)
ciliumAngiotensin-converting enzyme 2 Homo sapiens (human)
cell surfaceAngiotensin-converting enzyme 2 Homo sapiens (human)
membraneAngiotensin-converting enzyme 2 Homo sapiens (human)
apical plasma membraneAngiotensin-converting enzyme 2 Homo sapiens (human)
endocytic vesicle membraneAngiotensin-converting enzyme 2 Homo sapiens (human)
brush border membraneAngiotensin-converting enzyme 2 Homo sapiens (human)
membrane raftAngiotensin-converting enzyme 2 Homo sapiens (human)
extracellular exosomeAngiotensin-converting enzyme 2 Homo sapiens (human)
extracellular spaceAngiotensin-converting enzyme 2 Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (158)

Assay IDTitleYearJournalArticle
AID1676595Binding affinity to Ferric ion assessed as performance ratio ratio by measuring product of accounting ratio and retention ratio at 2.55 umol by immobilized metal-ion affinity chromatography2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID481446Effective permeability across human jejunum2010Journal of medicinal chemistry, May-13, Volume: 53, Issue:9
How well can the Caco-2/Madin-Darby canine kidney models predict effective human jejunal permeability?
AID481442Transcellular permeability at pH 6.5 calculated from in vitro P app values in Caco-2 and/or MDCK cells2010Journal of medicinal chemistry, May-13, Volume: 53, Issue:9
How well can the Caco-2/Madin-Darby canine kidney models predict effective human jejunal permeability?
AID38852In vitro inhibitory activity against Angiotensin I converting enzyme1985Journal of medicinal chemistry, Apr, Volume: 28, Issue:4
Angiotensin-converting enzyme inhibitors: synthesis and biological activity of acyl tripeptide analogues of enalapril.
AID781326pKa (acid-base dissociation constant) as determined by Avdeef ref: DOI: 10.1002/047145026X2014Pharmaceutical research, Apr, Volume: 31, Issue:4
Comparison of the accuracy of experimental and predicted pKa values of basic and acidic compounds.
AID444057Fraction escaping hepatic elimination in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1676589Binding affinity to Nickel cation assessed as performance ratio ratio by measuring product of accounting ratio and retention ratio at 2.55 umol by immobilized metal-ion affinity chromatography2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID540209Volume of distribution at steady state in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID425652Total body clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID481440Dissociation constant, pKa of the compound2010Journal of medicinal chemistry, May-13, Volume: 53, Issue:9
How well can the Caco-2/Madin-Darby canine kidney models predict effective human jejunal permeability?
AID1676593Binding affinity to Gallium ion assessed as retention ratio by measuring compound detected in elution fraction/total compound detected at 2.55 umol by immobilized metal-ion affinity chromatography2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID1474167Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID184243Maximum inhibitory effect on Angiotensin I induced pressor responses in anesthetized normotensive rats with 10 ug/kg dose of compound given intravenously1989Journal 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.
AID1676599Binding affinity to cupric ion assessed as accounting ratio by measuring total compound detected/total compound adsorbed at 2.55 umol by immobilized metal-ion affinity chromatography2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID1676592Binding affinity to Gallium ion assessed as performance ratio ratio by measuring product of accounting ratio and retention ratio at 2.55 umol by immobilized metal-ion affinity chromatography2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID444050Fraction unbound in human plasma2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1676600Binding affinity to zinc ion assessed as accounting ratio by measuring total compound detected/total compound adsorbed at 2.55 umol by immobilized metal-ion affinity chromatography2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID18861GOF value represents multisets of log P data1998Journal of medicinal chemistry, Dec-03, Volume: 41, Issue:25
Correlation of human jejunal permeability (in vivo) of drugs with experimentally and theoretically derived parameters. A multivariate data analysis approach.
AID444058Volume of distribution at steady state in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID26526Compound was tested for its maximum lipophilicity.1991Journal of medicinal chemistry, Jan, Volume: 34, Issue:1
Design, synthesis, and physicochemical properties of a novel, conformationally restricted 2,3-dihydro-1,3,4-thiadiazole-containing angiotensin converting enzyme inhibitor which is preferentially eliminated by the biliary route in rats.
AID21264Effective permeability measured in human.1998Journal of medicinal chemistry, Dec-03, Volume: 41, Issue:25
Correlation of human jejunal permeability (in vivo) of drugs with experimentally and theoretically derived parameters. A multivariate data analysis approach.
AID1473739Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID182320% Inhibition of angiotensin-I induced pressor response in normotensive rats after intravenous dosing of 0.05 umol/kg1988Journal of medicinal chemistry, Jun, Volume: 31, Issue:6
Angiotensin-converting enzyme inhibitors. Mercaptan, carboxyalkyl dipeptide, and phosphinic acid inhibitors incorporating 4-substituted prolines.
AID38101Compound tested in vivo for inhibition of Angiotensin I converting enzyme in rat1989Journal of medicinal chemistry, Jul, Volume: 32, Issue:7
Angiotensin converting enzyme inhibitors: spirapril and related compounds.
AID39763Time to inhibit maximum Angiotensin I converting enzyme in Hog plasma1990Journal of medicinal chemistry, Jun, Volume: 33, Issue:6
Angiotensin converting enzyme inhibitors. 10. Aryl sulfonamide substituted N-[1-carboxy-3-phenylpropyl]-L-alanyl-L-proline derivatives as novel antihypertensives.
AID15711Calculated partition coefficient (clogP)1998Journal of medicinal chemistry, Dec-03, Volume: 41, Issue:25
Correlation of human jejunal permeability (in vivo) of drugs with experimentally and theoretically derived parameters. A multivariate data analysis approach.
AID444055Fraction absorbed in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID182321% Inhibition of angiotensin-I induced pressor response in normotensive rats after intravenous dosing of 0.15 umol/kg1988Journal of medicinal chemistry, Jun, Volume: 31, Issue:6
Angiotensin-converting enzyme inhibitors. Mercaptan, carboxyalkyl dipeptide, and phosphinic acid inhibitors incorporating 4-substituted prolines.
AID24448Partition coefficient value and its ionic species.1998Journal of medicinal chemistry, Dec-03, Volume: 41, Issue:25
Correlation of human jejunal permeability (in vivo) of drugs with experimentally and theoretically derived parameters. A multivariate data analysis approach.
AID25867Ratio of biliary and urinary excretion of angiotensin converting enzyme inhibitors in male rat after intravenous dosing.1991Journal of medicinal chemistry, Jan, Volume: 34, Issue:1
Design, synthesis, and physicochemical properties of a novel, conformationally restricted 2,3-dihydro-1,3,4-thiadiazole-containing angiotensin converting enzyme inhibitor which is preferentially eliminated by the biliary route in rats.
AID186360Baseline mean aortic blood pressure in conscious renal (1clip/2kidney) hypertensive rats at dose 10 mg/kg administered orally.1986Journal of medicinal chemistry, Oct, Volume: 29, Issue:10
Synthesis of novel angiotensin converting enzyme inhibitor quinapril and related compounds. A divergence of structure-activity relationships for non-sulfhydryl and sulfhydryl types.
AID476929Human intestinal absorption in po dosed human2010European journal of medicinal chemistry, Mar, Volume: 45, Issue:3
Neural computational prediction of oral drug absorption based on CODES 2D descriptors.
AID37658In vitro activity against angiotensin I converting enzyme especially against Hip-His-Leu residues1991Journal of medicinal chemistry, Feb, Volume: 34, Issue:2
Configuration and preferential solid-state conformations of perindoprilat (S-9780). Comparison with the crystal structures of other ACE inhibitors and conclusions related to structure-activity relationships.
AID1466510Plasma protein binding in rat2017Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11
Approaches towards the development of chimeric DPP4/ACE inhibitors for treating metabolic syndrome.
AID37962In vitro inhibitory activity against angiotensin I converting enzyme of rats.1988Journal of medicinal chemistry, Jun, Volume: 31, Issue:6
Angiotensin-converting enzyme inhibitors. Mercaptan, carboxyalkyl dipeptide, and phosphinic acid inhibitors incorporating 4-substituted prolines.
AID186365Baseline mean aortic blood pressure in conscious renal (1clip/2kidney) hypertensive rats at dose 30 mg/kg administered orally.1986Journal of medicinal chemistry, Oct, Volume: 29, Issue:10
Synthesis of novel angiotensin converting enzyme inhibitor quinapril and related compounds. A divergence of structure-activity relationships for non-sulfhydryl and sulfhydryl types.
AID1466506Inhibition of ob/ob mouse plasma ACE2017Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11
Approaches towards the development of chimeric DPP4/ACE inhibitors for treating metabolic syndrome.
AID481441Aqueous diffusivity at 37C2010Journal of medicinal chemistry, May-13, Volume: 53, Issue:9
How well can the Caco-2/Madin-Darby canine kidney models predict effective human jejunal permeability?
AID444052Hepatic clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID540212Mean residence time in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID182330% Inhibition of angiotensin-I induced pressor response in normotensive rats after peroral dosing of 5 umol/kg1988Journal of medicinal chemistry, Jun, Volume: 31, Issue:6
Angiotensin-converting enzyme inhibitors. Mercaptan, carboxyalkyl dipeptide, and phosphinic acid inhibitors incorporating 4-substituted prolines.
AID37656Evaluation of in vitro inhibitory activity against Angiotensin I converting enzyme1995Journal of medicinal chemistry, Dec-22, Volume: 38, Issue:26
New alpha-thiol dipeptide dual inhibitors of angiotensin-I converting enzyme and neutral endopeptidase EC 3.4.24.11.
AID1676594Binding affinity to gallium ion assessed as accounting ratio by measuring total compound detected/total compound adsorbed at 2.55 umol by immobilized metal-ion affinity chromatography2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID1676597Binding affinity to cupric ion assessed as performance ratio ratio by measuring product of accounting ratio and retention ratio at 2.55 umol by immobilized metal-ion affinity chromatography2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID481444Octanol-water partition coefficient, log P of the compound2010Journal of medicinal chemistry, May-13, Volume: 53, Issue:9
How well can the Caco-2/Madin-Darby canine kidney models predict effective human jejunal permeability?
AID182328% Inhibition of angiotensin-I induced pressor response in normotensive rats after peroral dosing of 15 umol/kg1988Journal of medicinal chemistry, Jun, Volume: 31, Issue:6
Angiotensin-converting enzyme inhibitors. Mercaptan, carboxyalkyl dipeptide, and phosphinic acid inhibitors incorporating 4-substituted prolines.
AID37931In vitro inhibition of Angiotensin I converting enzyme in rabbit lung1990Journal of medicinal chemistry, Jun, Volume: 33, Issue:6
Angiotensin converting enzyme inhibitors. 10. Aryl sulfonamide substituted N-[1-carboxy-3-phenylpropyl]-L-alanyl-L-proline derivatives as novel antihypertensives.
AID540213Half life in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
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.
AID1466508Plasma protein binding in human2017Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11
Approaches towards the development of chimeric DPP4/ACE inhibitors for treating metabolic syndrome.
AID38859Compound was tested for its inhibitory potency against angiotensin I converting enzyme.1991Journal of medicinal chemistry, Feb, Volume: 34, Issue:2
Molecular and crystal structures of MDL27,467A hydrochloride and quinapril hydrochloride, two ester derivatives of potent angiotensin converting enzyme inhibitors.
AID1466502Inhibition of Wistar rat plasma DPP42017Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11
Approaches towards the development of chimeric DPP4/ACE inhibitors for treating metabolic syndrome.
AID425653Renal clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID177501In vivo inhibition of angiotensin I induced pressor effect after po administration in rats1988Journal of medicinal chemistry, Jan, Volume: 31, Issue:1
(Phosphinyloxy)acyl amino acid inhibitors of angiotensin converting enzyme (ACE). 1. Discovery of (S)-1-[6-amino-2-[[hydroxy(4-phenylbutyl)phosphinyl]oxy]-1-oxohexyl]-L -proline a novel orally active inhibitor of ACE.
AID37639Inhibition of Angiotensin I converting enzyme from pig renal cortex, 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.
AID1466504Inhibition of human plasma DPP42017Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11
Approaches towards the development of chimeric DPP4/ACE inhibitors for treating metabolic syndrome.
AID37646In vitro inhibition of angiotensin I converting enzyme in rabbit lung with hippuryl-histidyl-leucine as substrate1988Journal of medicinal chemistry, Jan, Volume: 31, Issue:1
(Phosphinyloxy)acyl amino acid inhibitors of angiotensin converting enzyme (ACE). 1. Discovery of (S)-1-[6-amino-2-[[hydroxy(4-phenylbutyl)phosphinyl]oxy]-1-oxohexyl]-L -proline a novel orally active inhibitor of ACE.
AID38089Inhibition of rat Angiotensin I converting enzyme (ACE), using Hip-Gly-Gly as synthetic substrate.1987Journal of medicinal chemistry, Jun, Volume: 30, Issue:6
Synthesis and structure-activity relationships of potent new angiotensin converting enzyme inhibitors containing saturated bicyclic amino acids.
AID177500In vivo inhibition of angiotensin I induced pressor effect after iv administration in rats1988Journal of medicinal chemistry, Jan, Volume: 31, Issue:1
(Phosphinyloxy)acyl amino acid inhibitors of angiotensin converting enzyme (ACE). 1. Discovery of (S)-1-[6-amino-2-[[hydroxy(4-phenylbutyl)phosphinyl]oxy]-1-oxohexyl]-L -proline a novel orally active inhibitor of ACE.
AID26306Logarithm of the ratio of anionic to unionized species at pH 7.41991Journal of medicinal chemistry, Jan, Volume: 34, Issue:1
Design, synthesis, and physicochemical properties of a novel, conformationally restricted 2,3-dihydro-1,3,4-thiadiazole-containing angiotensin converting enzyme inhibitor which is preferentially eliminated by the biliary route in rats.
AID182319% Inhibition of angiotensin-I induced pressor response in normotensive rats after intravenous dosing of 0.015 umol/kg1988Journal of medicinal chemistry, Jun, Volume: 31, Issue:6
Angiotensin-converting enzyme inhibitors. Mercaptan, carboxyalkyl dipeptide, and phosphinic acid inhibitors incorporating 4-substituted prolines.
AID186362Baseline mean aortic blood pressure in conscious renal (1clip/2kidney) hypertensive rats at dose 1 mg/kg administered orally.1986Journal of medicinal chemistry, Oct, Volume: 29, Issue:10
Synthesis of novel angiotensin converting enzyme inhibitor quinapril and related compounds. A divergence of structure-activity relationships for non-sulfhydryl and sulfhydryl types.
AID681152TP_TRANSPORTER: uptake in Xenopus laevis oocytes2002Drug metabolism and pharmacokinetics, , Volume: 17, Issue:4
Transporter-mediated Drug Interactions.
AID24202Distribution coefficient in octanol/water at pH 5.51998Journal of medicinal chemistry, Dec-03, Volume: 41, Issue:25
Correlation of human jejunal permeability (in vivo) of drugs with experimentally and theoretically derived parameters. A multivariate data analysis approach.
AID1676602Binding affinity to ferric ion assessed as accounting ratio by measuring total compound detected/total compound adsorbed at 2.55 umol by immobilized metal-ion affinity chromatography2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID39622Inhibition of Angiotensin I converting enzyme (ACE) in Bothrops jararaca venom2002Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26
2002 Alfred Burger Award Address in Medicinal Chemistry. Natural products and design: interrelated approaches in drug discovery.
AID1466505Inhibition of Wistar rat plasma ACE2017Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11
Approaches towards the development of chimeric DPP4/ACE inhibitors for treating metabolic syndrome.
AID444056Fraction escaping gut-wall elimination in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1466507Inhibition of human plasma ACE2017Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11
Approaches towards the development of chimeric DPP4/ACE inhibitors for treating metabolic syndrome.
AID38864Inhibitory concentration against Angiotensin I converting enzyme1986Journal of medicinal chemistry, Feb, Volume: 29, Issue:2
Conformationally restricted inhibitors of angiotensin converting enzyme: synthesis and computations.
AID39750In vitro inhibitory activity against Angiotensin I converting enzyme from unpurified guinea pig serum1985Journal of medicinal chemistry, Sep, Volume: 28, Issue:9
Synthesis and biological activity of modified peptide inhibitors of angiotensin-converting enzyme.
AID39759Time during which Angiotensin I converting enzyme inhibition is greater than or equal to 30% in Hog plasma1990Journal of medicinal chemistry, Jun, Volume: 33, Issue:6
Angiotensin converting enzyme inhibitors. 10. Aryl sulfonamide substituted N-[1-carboxy-3-phenylpropyl]-L-alanyl-L-proline derivatives as novel antihypertensives.
AID1474166Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID186366Baseline mean aortic blood pressure in conscious renal (1clip/2kidney) hypertensive rats at dose 3 mg/kg administered orally.1986Journal of medicinal chemistry, Oct, Volume: 29, Issue:10
Synthesis of novel angiotensin converting enzyme inhibitor quinapril and related compounds. A divergence of structure-activity relationships for non-sulfhydryl and sulfhydryl types.
AID38849Inhibition of angiotensin I converting enzyme in silico1997Journal of medicinal chemistry, Sep-26, Volume: 40, Issue:20
Validation of EGSITE2, a mixed integer program for deducing objective site models for experimental binding data.
AID24203Distribution coefficient in octanol/water at pH 6.51998Journal of medicinal chemistry, Dec-03, Volume: 41, Issue:25
Correlation of human jejunal permeability (in vivo) of drugs with experimentally and theoretically derived parameters. A multivariate data analysis approach.
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.
AID682027TP_TRANSPORTER: uptake in Oatp1-expressing HeLa cells1998Hepatology (Baltimore, Md.), Nov, Volume: 28, Issue:5
The modified dipeptide, enalapril, an angiotensin-converting enzyme inhibitor, is transported by the rat liver organic anion transport protein.
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.
AID1676596Binding affinity to Ferric ion assessed as retention ratio by measuring compound detected in elution fraction/total compound detected at 2.55 umol by immobilized metal-ion affinity chromatography2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID1473741Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID444054Oral bioavailability in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1676590Binding affinity to Nickel cation assessed as retention ratio by measuring compound detected in elution fraction/total compound detected at 2.55 umol by immobilized metal-ion affinity chromatography2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID186677Maximum change aortic blood pressure in conscious renal (1clip/2kidney) hypertensive rats at dose 1 mg/kg administered orally at 9 hr.1986Journal of medicinal chemistry, Oct, Volume: 29, Issue:10
Synthesis of novel angiotensin converting enzyme inhibitor quinapril and related compounds. A divergence of structure-activity relationships for non-sulfhydryl and sulfhydryl types.
AID186685Maximum change aortic blood pressure in conscious renal (1clip/2kidney) hypertensive rats at dose 3 mg/kg administered orally at 2 hr.1986Journal of medicinal chemistry, Oct, Volume: 29, Issue:10
Synthesis of novel angiotensin converting enzyme inhibitor quinapril and related compounds. A divergence of structure-activity relationships for non-sulfhydryl and sulfhydryl types.
AID37930Concentration required for 50% inhibition of rabbit lung Angiotensin I converting enzyme with 5 mM hippuryl-histidyl-leucine as substrate1988Journal of medicinal chemistry, Feb, Volume: 31, Issue:2
Angiotensin-converting enzyme inhibitors. 2. Perhydroazepin-2-one derivatives.
AID1466503Inhibition of ob/ob mouse plasma DPP42017Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11
Approaches towards the development of chimeric DPP4/ACE inhibitors for treating metabolic syndrome.
AID24420Partition coefficient (logP)1998Journal of medicinal chemistry, Dec-03, Volume: 41, Issue:25
Correlation of human jejunal permeability (in vivo) of drugs with experimentally and theoretically derived parameters. A multivariate data analysis approach.
AID444053Renal clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID26611pKa value of the compound. (extrapolated values)1998Journal of medicinal chemistry, Dec-03, Volume: 41, Issue:25
Correlation of human jejunal permeability (in vivo) of drugs with experimentally and theoretically derived parameters. A multivariate data analysis approach.
AID1676591Binding affinity to Nickel cation assessed as accounting ratio by measuring total compound detected/total compound adsorbed at 2.55 umol by immobilized metal-ion affinity chromatography2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID1676588Binding affinity to Zinc ion assessed as performance ratio ratio by measuring product of accounting ratio and retention ratio at 2.55 umol by immobilized metal-ion affinity chromatography2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID540211Fraction unbound in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID37671Inhibitory activity against rabbit lung Angiotensin I converting enzyme with 5 mM hippuryl-histidyl-leucine as substrate1987Journal of medicinal chemistry, Nov, Volume: 30, Issue:11
Angiotensin-converting enzyme inhibitors: perhydro-1,4-thiazepin-5-one derivatives.
AID1676598Binding affinity to cupric ion assessed as retention ratio by measuring compound detected in elution fraction/total compound detected at 2.55 umol by immobilized metal-ion affinity chromatography2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID540210Clearance in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID481439Absolute bioavailability in human2010Journal of medicinal chemistry, May-13, Volume: 53, Issue:9
How well can the Caco-2/Madin-Darby canine kidney models predict effective human jejunal permeability?
AID39761In vitro inhibition of Angiotensin I converting enzyme in Hog plasma1990Journal of medicinal chemistry, Jun, Volume: 33, Issue:6
Angiotensin converting enzyme inhibitors. 10. Aryl sulfonamide substituted N-[1-carboxy-3-phenylpropyl]-L-alanyl-L-proline derivatives as novel antihypertensives.
AID37801Inhibitory activity against rabbit lung angiotensin-1 converting enzyme1988Journal of medicinal chemistry, Jun, Volume: 31, Issue:6
Angiotensin-converting enzyme inhibitors. Mercaptan, carboxyalkyl dipeptide, and phosphinic acid inhibitors incorporating 4-substituted prolines.
AID186544Maximum change aortic blood pressure in conscious renal (1clip/2kidney) hypertensive rats at dose 10 mg/kg administered orally at 6 hr.1986Journal of medicinal chemistry, Oct, Volume: 29, Issue:10
Synthesis of novel angiotensin converting enzyme inhibitor quinapril and related compounds. A divergence of structure-activity relationships for non-sulfhydryl and sulfhydryl types.
AID38847Binding affinity towards Angiotensin I converting enzyme of rat brain IgG immobilized enzyme.1985Journal of medicinal chemistry, Sep, Volume: 28, Issue:9
Synthesis and biological evaluation of phosphonamidate peptide inhibitors of enkephalinase and angiotensin-converting enzyme.
AID1466509Plasma protein binding in mouse2017Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11
Approaches towards the development of chimeric DPP4/ACE inhibitors for treating metabolic syndrome.
AID25872The acid dissociation constant, pKa was determined.'a' represents value of C-terminus carboxylic acid.1991Journal of medicinal chemistry, Jan, Volume: 34, Issue:1
Design, synthesis, and physicochemical properties of a novel, conformationally restricted 2,3-dihydro-1,3,4-thiadiazole-containing angiotensin converting enzyme inhibitor which is preferentially eliminated by the biliary route in rats.
AID24204Distribution coefficient in octanol/water at pH 7.41998Journal of medicinal chemistry, Dec-03, Volume: 41, Issue:25
Correlation of human jejunal permeability (in vivo) of drugs with experimentally and theoretically derived parameters. A multivariate data analysis approach.
AID1473740Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 10 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID38853Compound tested in vitro for inhibition of Angiotensin I converting enzyme1989Journal of medicinal chemistry, Jul, Volume: 32, Issue:7
Angiotensin converting enzyme inhibitors: spirapril and related compounds.
AID1473738Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID444051Total clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID38086Compound was tested for inhibitory activity against angiotensin I converting enzyme1991Journal of medicinal chemistry, Jan, Volume: 34, Issue:1
Design, synthesis, and physicochemical properties of a novel, conformationally restricted 2,3-dihydro-1,3,4-thiadiazole-containing angiotensin converting enzyme inhibitor which is preferentially eliminated by the biliary route in rats.
AID37939In vivo inhibition of Angiotensin I converting enzyme in rabbit lung after (po) administration of a dose of 10(mg/kg)1990Journal of medicinal chemistry, Jun, Volume: 33, Issue:6
Angiotensin converting enzyme inhibitors. 10. Aryl sulfonamide substituted N-[1-carboxy-3-phenylpropyl]-L-alanyl-L-proline derivatives as novel antihypertensives.
AID39616Inhibition of Angiotensin I converting enzyme1993Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15
Excursions in drug discovery.
AID39758Inhibition of guinea pig angiotensin I converting enzyme1986Journal of medicinal chemistry, Oct, Volume: 29, Issue:10
Synthesis of novel angiotensin converting enzyme inhibitor quinapril and related compounds. A divergence of structure-activity relationships for non-sulfhydryl and sulfhydryl types.
AID186682Maximum change aortic blood pressure in conscious renal (1clip/2kidney) hypertensive rats at dose 30 mg/kg administered orally at 6 hr.1986Journal of medicinal chemistry, Oct, Volume: 29, Issue:10
Synthesis of novel angiotensin converting enzyme inhibitor quinapril and related compounds. A divergence of structure-activity relationships for non-sulfhydryl and sulfhydryl types.
AID1676601Binding affinity to Zinc ion assessed as retention ratio by measuring compound detected in elution fraction/total compound detected at 2.55 umol by immobilized metal-ion affinity chromatography2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID1449628Inhibition of human BSEP expressed in baculovirus transfected fall armyworm Sf21 cell membranes vesicles assessed as reduction in ATP-dependent [3H]-taurocholate transport into vesicles incubated for 5 mins by Topcount based rapid filtration method2012Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12
Mitigating the inhibition of human bile salt export pump by drugs: opportunities provided by physicochemical property modulation, in silico modeling, and structural modification.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID1745845Primary qHTS for Inhibitors of ATXN expression
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.
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.
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.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID1347151Optimization of GU AMC 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.
AID1347410qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library2019Cellular signalling, 08, Volume: 60A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening.
AID1347058CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347405qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC 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.
AID1347059CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347057CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
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.
AID1345457Human Angiotensin-converting enzyme (M2: Angiotensin-converting (ACE and ACE2))1994Journal of cardiovascular pharmacology, , Volume: 23 Suppl 4Compared properties of trandolapril, enalapril, and their diacid metabolites.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).2014Journal of biomolecular screening, Jul, Volume: 19, Issue:6
A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (788)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990169 (21.45)18.7374
1990's376 (47.72)18.2507
2000's156 (19.80)29.6817
2010's69 (8.76)24.3611
2020's18 (2.28)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 7.69

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

MetricThis Compound (vs All)
Research Demand Index7.69 (24.57)
Research Supply Index6.86 (2.92)
Research Growth Index4.55 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (7.69)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials109 (12.88%)5.53%
Reviews21 (2.48%)6.00%
Case Studies15 (1.77%)4.05%
Observational0 (0.00%)0.25%
Other701 (82.86%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]