Page last updated: 2024-11-06

methyldopa

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Description

Methyldopa is a medication used to treat high blood pressure. It is a prodrug that is converted to alpha-methylnorepinephrine, which then acts as a false neurotransmitter at alpha-2 adrenergic receptors in the brainstem. This leads to decreased sympathetic nervous system activity, resulting in a decrease in blood pressure. Methyldopa is a relatively safe and effective medication for the treatment of high blood pressure, particularly in pregnant women and patients with other medical conditions. It was first synthesized in the 1950s and has been widely used since then. Methyldopa is studied extensively to investigate its effects on different organ systems, potential side effects, and interactions with other medications. It is also studied to develop new and improved medications for the treatment of high blood pressure and other conditions.'

Methyldopa: An alpha-2 adrenergic agonist that has both central and peripheral nervous system effects. Its primary clinical use is as an antihypertensive agent. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

alpha-methyl-L-dopa : A derivative of L-tyrosine having a methyl group at the alpha-position and an additional hydroxy group at the 3-position on the phenyl ring. [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 CID38853
CHEMBL ID459
CHEBI ID61058
SCHEMBL ID34003
MeSH IDM0013626
PubMed CID38852
CHEMBL ID1591707
MeSH IDM0013626

Synonyms (357)

Synonym
BIDD:GT0620
AB01275508-01
methyldopum
metildopa
nci-c55721
methoplain
nsc-169916
l-methyldopa
l-(-)-3-(3,4-dihydroxyphenyl)-2-methylalanine
2-methyl-3-(3,4-dihydroxyphenyl)alanine
nr.c 2294
sembrina
mk. b51
dopatec
(-)-.alpha.-methyldopa
medomet
aldomin
amd
(-)-methyldopa
.alpha.-methyl-l-3,4-dihydroxyphenylalanine
baypresol
mk 351
becanta
sedometil
hypolag
alpha medopa
medopal
.alpha.-methyl-l-dopa
l-.alpha.-methyldopa
nsc169916
(s)-(-)-.alpha.-methyldopa
alphamethyldopa
aldometil
l-tyrosine, 3-hydroxy-.alpha.-methyl-
dopamethyperpax
bayer 1440 l
grospisk
dopamet
presolisin
smr000059170
3-(3,4-dihydroxyphenyl)-2-methyl-l-alanine
MLS000028644 ,
KBIO1_000142
DIVK1C_000142
3-hydroxy-alpha-methyl-l-tyrosine
EU-0100853
SPECTRUM_000937
BSPBIO_002021
methyldopa (l,-)
PRESTWICK_732
tocris-0584
cas-555-30-6
NCGC00024667-01
LOPAC0_000853
SPECTRUM5_001295
BPBIO1_000365
IDI1_000142
PRESTWICK2_000326
BSPBIO_000331
hyperpax
(2s)-2-amino-3-(3,4-dihydroxyphenyl)-2-methyl-propanoic acid
3-hydroxy-.alpha.-methyl-l-tyrosine
alpha-methyl-beta-(3,4-dihydroxyphenyl)-l-alanine
alpha-methyl-l-3,4-dihydroxyphenylalanine
alanine, 3-(3,4-dihydroxyphenyl)-2-methyl-, l-(-)-
metildopa [inn-spanish]
l(-)-beta-(3,4-dihydroxyphenyl)-alpha-methylalanine
l-(-)-alpha-methyl-beta-(3,4-dihydroxyphenyl)alanine
l-tyrosine, 3-hydroxy-alpha-methyl-
methyldopum [inn-latin]
levo-3-(3,4-dihydroxyphenyl)-2-methylalanine
l-alpha-methyl-3,4-dihydroxyphenylalanine
nsc 169916
l-2-amino-2-methyl-3-(3,4-dihydroxyphenyl)propionic acid
alpha-methyldopa (van)
dopegit
l-(alpha-md)
methyl-l-dopa
l-3-(3,4-dihydroxyphenyl)-2-methylalanine
ccris 4671
methyldopa (anhydrous)
hsdb 218
einecs 209-089-2
alpha-methyldihydroxyphenylalanine
methyldopa anhydrous
C07194
555-30-6
methyldopa
l-methyl dopa
alpha-methyl-l-dopa
l-alpha-methyldopa
alpha-methyl dopa
(s)-(-)-alpha-methyldopa
DB00968
anhydrous methyldopa
c10h13no4
KBIO2_001417
KBIO2_006553
KBIOSS_001417
KBIOGR_000547
KBIO3_001521
KBIO2_003985
SPBIO_001056
SPECTRUM2_001068
SPECTRUM4_000054
NINDS_000142
PRESTWICK0_000326
SPECTRUM3_000501
SPBIO_002252
PRESTWICK1_000326
SPECTRUM1500403
methyl dopa
PRESTWICK3_000326
NCGC00024667-05
NCGC00024667-03
NCGC00024667-06
NCGC00024667-02
l-alpha-methyl dopa
nu-medopa
alpha methyl l dopa
alpha methyldopa
apo-methyldopa
ALPHA-METHYLDOPA ,
mk-351; methyldopa
HMS2091F04
HMS2090B11
AC-11671
NCGC00024667-08
(2s)-2-amino-3-(3,4-dihydroxyphenyl)-2-methylpropanoic acid
nsc-760080
methyldopa (levorotatory)
bayer-1440l
j9.247i ,
methyldopa, anhydrous
CHEMBL459
chebi:61058 ,
mk-351
methyldopa (inn)
D08205
HMS500H04
88620-56-8
l-(-)-alpha-methyldopa
D1817
HMS1920N09
HMS1569A13
NCGC00024667-11
NCGC00024667-10
NCGC00024667-09
NCGC00024667-07
(2s)-2-azaniumyl-3-(3,4-dihydroxyphenyl)-2-methylpropanoate
HMS3262L07
HMS2096A13
tox21_202610
NCGC00260158-01
dtxcid403295
dtxsid5023295 ,
nsc760080
pharmakon1600-01500403
HMS2235N11
AKOS015960582
CCG-40120
novomedopa
methyldopa [inn]
m4r0h12f6m ,
unii-m4r0h12f6m
NCGC00024667-13
3-(3,4-dihydroxyphenyl)-2-methyl-l-alanine sesquihydrate
LP00853
(-)-.alpha.-methyl-3,4-dihydroxyphenylalanine
anhydrous methyldopa [mart.]
carbidopa impurity a [ep impurity]
methyldopa [hsdb]
methyldopa [who-dd]
lederdopa
methyldopa [mi]
l-.alpha.-methyl-3-(3,4)-dihydroxyphenylalanine
EPITOPE ID:146097
S1642
tyrosine, 3-hydroxy-.alpha.-methyl-
HMS3372J14
gtpl5217
DL-443
HY-B0225
MLS006011978
SCHEMBL34003
tox21_500853
NCGC00261538-01
5-amino-2-fluorophenylboronicacid
W-105555
Q-201392
bdbm48449
cid_38853
KS-1424
(-)-alpha-methyl-3,4-dihydroxyphenylalanine
l-(-)-?-methyldopa
3-(3,4-dihydroxyphenyl)-?-methyl-l-alanine
aldomine
alanine, 3-(3,4-dihydroxyphenyl)-2-methyl-, l-
3,4-dihydroxy-2-methylphenylalanine #
(s)-2-amino-3-(3,4-dihydroxyphenyl)-2-methylpropanoic acid
AB01275508_02
AB00052043_09
l-(-)-afae'a centa' nota inverted exclamation markafasa'a|afae'adaggeratrade mark?-methyldopa
l-(-)-a-methyldopa
SR-01000597712-3
sr-01000597712
SR-01000597712-1
AC-8431
medoba
methyldopa, united states pharmacopeia (usp) reference standard
methyldopa, european pharmacopoeia (ep) reference standard
methyldopa for system suitability, european pharmacopoeia (ep) reference standard
3-(3,4-dihydroxyphenyl)-2-methyl-l-alanine (h-l-ametyr(3-oh)-oh)
mfcd00004186
HMS3713A13
l-(-)-3-(3,4-dihydroxyphenyl)-2-methyl-alanine
l(-)-a-methylalanine
l-(-)-a-methyl-a-methyl-aldomin
a-methyldopa (van)
apo methyldopa tab 125mg
apo methyldopa tab 250mg
nu-medopa tab 125mg
3,4-dihydroxy-2-methylphenylalanine (acd/name 4.0)
a-methyl-l-3,4-dihydroxyphenylalanine
l-alpha-methyl-(3, 4-dihydroxyphenyl)alanine
l-a-methyldopa
l-a-methyl-(3, 4-dihydroxyphenyl)alanine
apo methyldopa tab 500mg
a-methyl-l-dopa
novo-medopa tab 250mg
a-methyl dopa
(s)-(-)-a-methyldopa
l-(a-md)
nu-medopa tab 250mg
methyldopa 250 tab
nu-medopa tab 500mg
methyldopa 500 tab 500mg
l(-)-alpha-methylalanine
l-(-)-alpha-methyl-alpha-methyl-aldomin
novo-medopa tab 125mg
(-)-a-methyldopa
methyldopa 125 tab 125mg
(-)-alpha-methyldopa
novo-medopa tab 500mg
mk-351;methyldopa
HB1822
3-(3,4-dihydroxyphenyl)-alpha-methyl-l-a lanine
Q412621
methyldopa (aldomet)
HMS3675G18
AS-13052
l-(-)--methyldopa
HMS3411G18
EN300-120685
SDCCGSBI-0050829.P002
NCGC00024667-21
HMS3887I15
l-(-)- alpha-methyldopa
D82313
l-(-)- alpha -methyldopa
mk-35
27289-76-5
(s)-2-amino-3-(3,4-dihydroxyphenyl)-2-methylpropanoicacid
Z1508915075
alpha-methyldopa, l-
mk b51
c02ab01
methyldopa (ep monograph)
nrc 2294
methyldopa (usp-rs)
2-amino-3-(3,4-dihydroxyphenyl)-2-methylpropionic acid
amodopa
l-alpha-methyl-3-(3,4)-dihydroxyphenylalanine
l-3,4-dihydroxy-alpha-methylphenylalanine
methyldopa (usp monograph)
methyldopa sesquihydrate (mart.)
l-(-)-beta-(3,4-dihydroxyphenyl)-alpha-methylalanine
l-3,4-dihydroxyphenyl-2-methylalanine
methyldopate hydrochloride (ester)
anhydrous methyldopa (mart.)
l-2-amino-2-amino-2-methyl-3-(3,4-dihydroxyphenyl)propionic acid sesquihydrate
methyldopa (mart.)
carbidopa impurity a (ep impurity)
methyldopate (ester)
bayer 1440l
(s)-alpha-methyldopa
3-hydroxy-alpha-methyl-l-tyrosine sesquihydrate
dopegyt
aldomet
medopren
presinol
3-hydroxy-alpha-methyl-l-tyrosine trihydrate
alpha-methyldopa sesquihydrate
l-tyrosine, 3-hydroxy-alpha-methyl-, hydrate (2:3)
ccris 1662
methyldopa 1.5-wasser
methyldopa sequihydrate
methyl dopa sesquihydrate
l-tyrosine, 3-hydroxy-alpha-methyl-, sesquihydrate
l-3-(3,4-dihydroxyphenyl)-2-methylalanine sesquihydrate
(-)-3-(3,4-dihydroxyphenyl)-2-methyl-l-alanine sesquihydrate, 99%
aldomet (tn)
methyldopa (usp)
41372-08-1
D00405
methyldopa hydrate (jp17)
NCGC00024667-04
methyldopa sesquihydrate
methyldopa hydrate
NCGC00259580-01
tox21_202031
tox21_300482
NCGC00254451-01
tox21_110917
cas-41372-08-1
dtxsid5020863 ,
dtxcid90863
56lh93261y ,
nsc 760080
unii-56lh93261y
methyldopa [usan:usp:inn:ban:jan]
S5954
(-)-3-(3,4-dihydroxyphenyl)-2-methyl-l-alanine sesquihydrate
methyldopa [usan]
l-tyrosine, 3-hydroxy-.alpha.-methyl-, hydrate (2:3)
methyldopa [usp-rs]
methyldopa [orange book]
methyldopa sesquihydrate [mi]
methyldopa sesquihydrate [who-dd]
l-tyrosine, 3-hydroxy-.alpha.-methyl-, sesquihydrate
aldoril component methyldopa
methyldopa component of aldoril
methyldopum [who-ip latin]
methyldopa [mart.]
methyldopa [ep monograph]
methyldopa [usp monograph]
methyldopa hydrate [jan]
methyldopa sesquihydrate [mart.]
methyldopa [who-ip]
methyldopa [vandf]
NCGC00024667-14
tox21_110917_1
YKFCISHFRZHKHY-NGQGLHOPSA-N
CHEMBL1591707
mfcd30179484
methyldopa sesquihydrate; (2s)-2-amino-3-(3,4-dihydroxyphenyl)-2-methylpropanoic acid sesquihydrate; l-methyldopa sesquihydrate, 3-hydroxy-?-methyl-l-tyrosine hydrate (2:3); carbidopa imp. a (ep); carbidopa impurity a as sesquihydrate
(s)-2-amino-3-(3,4-dihydroxyphenyl)-2-methylpropanoic acid sesquihydrate
methyldopa hydrate (1:1.5)
EN300-1692905
bis((2s)-2-amino-3-(3,4-dihydroxyphenyl)-2-methylpropanoic acid) trihydrate
l-(-)-|a-methyldopa hydrate
mk-351 hydrate
l-(-)-a-methyldopa hydrate
D87780
l-alpha-methyl-dopa middot sesquihydrate
l-?-methyl dopa hydrate
AKOS040758837

Research Excerpts

Toxicity

Maternal beta-blockade with labetalol is as safe as methyldopa for the fetus and the newborn. Clonidine hydrochloride appears to be a safe antihypertensive agent in pregnancy.

ExcerptReferenceRelevance
" The elderly are probably more sensitive than younger patients to the adverse effects of antihypertensive drugs, for various reasons, among which are age- and disease-related changes that can lead to altered pharmacodynamics and pharmacokinetics."( Potential adverse effects of antihypertensive drugs in the elderly.
Lamy, PP, 1988
)
0.27
" These data indicate that maternal beta-blockade with labetalol is as safe as methyldopa for the fetus and the newborn."( Comparison of antihypertensive efficacy and perinatal safety of labetalol and methyldopa in the treatment of hypertension in pregnancy: a randomized controlled trial.
Breart, G; Maillard, F; Papiernik, E; Plouin, PF; Relier, JP, 1988
)
0.27
" Labetalol is safe to the fetus and newborn and might offer a better prevention of intrauterine death than methyldopa."( [Maternal effects and perinatal safety of labetalol in the treatment of hypertension in pregnancy. Comparison with methyldopa in a randomized cooperative trial].
Bréart, G; Maillard, F; Papiernik, E; Plouin, PF; Relier, JP, 1987
)
0.27
" The basis of this noncompliance is multifactorial, but a large component is related to the adverse symptoms produced by the commonly prescribed antihypertensive agents."( Utility of behavioral science techniques in assessing adverse effects of antihypertensive agents.
Williams, GH, 1987
)
0.27
" Clonidine hydrochloride, like methyldopa, appears to be a safe antihypertensive agent in pregnancy."( Clonidine hydrochloride--a safe and effective antihypertensive agent in pregnancy.
Child, A; Henderson-Smart, DJ; Horvath, JS; Korda, A; Phippard, A; Tiller, DJ, 1985
)
0.27
" A discussion on the pharmacological basis of the side effects of the centrally acting antihypertensives has been limited to those adverse reactions that are somehow related to alpha-adrenergic receptors."( The hypotensive activity and side effects of methyldopa, clonidine, and guanfacine.
Thoolen, MJ; Timmermans, PB; van Zwieten, PA,
)
0.13
" Enalapril has a good safety profile as measured by frequency of clinical and laboratory adverse experiences."( The efficacy and safety of enalapril in moderate to severe essential hypertension.
Kramsch, DM; Kulaga, SF; Walker, JF, 1984
)
0.27
" Other reported effects are toxic confusional states and psychotic reactions."( Psychiatric side effects of antihypertensive drugs other than reserpine.
Fleminger, R; Paykel, ES; Watson, JP, 1982
)
0.26
" LD50 studies in mice have established that 6-OH-alpha-Me-Dopa is over four times more toxic than alpha-Me-Dopa."( Synthetic and preliminary hemodynamic and whole animal toxicity studies on (R,S)-, (R)-, and (S)-2-methyl-3-(2,4,5-trihydroxyphenyl)alanine.
Castagnoli, N; Cheng, A; Karashima, D; Melmon, KL; Musson, DG; Rubiero, H, 1980
)
0.26
" Although methyldopa is considered to have a wide margin of safety in the treatment of chronic hypertension in pregnancy, potentially serious adverse effects can occur."( Methyldopa hepatotoxicity in pregnancy: a case report.
Piercy, WN; Smith, GN, 1995
)
0.29
"5 million adverse drug reaction (ADR) reports for 8620 drugs/biologics that are listed for 1191 Coding Symbols for Thesaurus of Adverse Reaction (COSTAR) terms of adverse effects."( Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
Benz, RD; Contrera, JF; Kruhlak, NL; Matthews, EJ; Weaver, JL, 2004
)
0.32
" An understanding of structure-activity relationships (SARs) of chemicals can make a significant contribution to the identification of potential toxic effects early in the drug development process and aid in avoiding such problems."( Developing structure-activity relationships for the prediction of hepatotoxicity.
Fisk, L; Greene, N; Naven, RT; Note, RR; Patel, ML; Pelletier, DJ, 2010
)
0.36
"Chronic hypertension is associated with adverse perinatal outcomes, although the optimal treatment is unclear."( Comparative efficacy and safety of oral antihypertensive agents in pregnant women with chronic hypertension: a network metaanalysis.
Bellos, I; Daskalakis, G; Loutradis, D; Papapanagiotou, A; Pergialiotis, V, 2020
)
0.56
"The primary outcome was the number of adverse events that occurred after the administration of magnesium sulphate and/or methyldopa to pregnant women by CHWs."( The ability and safety of community-based health workers to safely initiate lifesaving therapies for pre-eclampsia in Ogun State, Nigeria: An analysis of 260 community treatments with MgSO
Adepoju, AA; Adetoro, OO; Akadri, AA; Akeju, DO; Bhutta, Z; Dada, OA; Drebit, S; Jaiyesimi, E; Li, L; Magee, LA; Nathan, HL; Nwankpa, CC; Odubena, OO; Payne, B; Sharma, S; Shennan, AH; Sotunsa, J; Soyinka, O; Tu, D; Vidler, M; von Dadelszen, P, 2021
)
0.62

Pharmacokinetics

Methyldopa has bi-phasic elimination after both intravenous and oral administration. Half-life of the alpha-phase is 0.

ExcerptReferenceRelevance
" Pharmacokinetic variables have been determined that allow: (1) derivation of the loading dose necessary to achieve rapid control of blood pressure with propranolol hydrochloride, guanethidine, minoxidil and clonidine hydrochloride; (2) reduced frequency of dosing with methyldopa, hydralazine hydrochloride, prazosin hydrochloride, propranolol and clonidine; and (3) alteration of propranolol and hydralazine dosage based on physiologic factors (e."( Using pharmacokinetics in drug therapy. V: Contributions to developing dosage regimens for antihypertensive drugs.
Schumacher, GE, 1979
)
0.26
" Absorption profiles were constructed with the aid of the pharmacokinetic model and contrasted with estimates of absorption which were model-independent."( Pharmacokinetics of methyldopa in man.
Baer, JE; Breault, GO; Foltz, EL; Kwan, KC; Totaro, JA, 1976
)
0.26
") pharmacokinetic profile of two controlled-release products of levodopa (Madopar HBS and Sinemet CR) was compared to conventional Madopar capsules in 18 healthy volunteers in a cross-over, randomized design."( Comparative multiple-dose pharmacokinetics of controlled-release levodopa products.
Collin, C; Eckernäs, SA; Grahnén, A; Ling-Andersson, A; Nilsson, M; Tiger, G, 1992
)
0.28
" These alpha MD kinetic analyses illustrate the adaptation of AH and CSF removal procedures to the pharmacokinetic studies of the brain and ocular entry of AA isomers."( Comparative pharmacokinetics of D- and L-alphamethyldopa in plasma, aqueous humor, and cerebrospinal fluid in rabbits.
Auclair, E; Chaouloff, F; Elghozi, JL; Laude, D; Wainer, IW, 1988
)
0.27
" As the basis of conclusive human pharmacokinetic and bioavailability/bioequivalence studies is a validated analytical method, which is reliable, selective, sensitive and able to proceed hundreds or even thousands of samples in a limited time, an assay to fulfill these needs was developed."( Determination of methyldopa in plasma using high-performance liquid chromatography with electrochemical detection. Application to pharmacokinetic/bioavailability studies.
Dilger, C; Jaeger, H; Salama, Z, 1987
)
0.27
"Statistical methods for validating assays used in pharmacokinetic studies are discussed."( Validation of assay methodology used in pharmacokinetic studies.
Aarons, L; Rowland, M; Toon, S, 1987
)
0.27
" 163) on the serum t1/2 and other pharmacokinetic parameters of co-administered L-3,4-dihydroxyphenylalanine (L-DOPA) were compared to those of the reversible inhibitor, carbidopa in rats."( A comparison of the effects of reversible and irreversible inhibitors of aromatic L-amino acid decarboxylase on the half-life and other pharmacokinetic parameters of oral L-3,4-dihydroxyphenylalanine.
Haegele, KD; Huebert, ND; Palfreyman, MG,
)
0.13
" A temporal variation of the kinetics of both L-dopa and carbidopa was demonstrated with higher plasma clearance and lower area under concentration curve after the administration at 2200 hours."( Circadian phase dependent pharmacokinetics of L-dopa, its main metabolites (3-OMD, HVA, DOPAC) and carbidopa in rats.
Andre, MH; Bruguerolle, B; Grignon, S, 1996
)
0.29
"The aim of this study was to assess the pharmacokinetics and subsequent pharmacodynamic interaction of MPC-1304, a dihydropyridine Ca2+ antagonist, with other drugs in animal experiments."( Interaction of some drugs on the pharmacokinetics or pharmacodynamics of MPC-1304, a dihydropyridine Ca2+ antagonist.
Miyake, H; Miyoshi, K; Nakano, M; Nishizaki, J; Umeno, Y; Yoshida, K,
)
0.13
" Plasma concentrations of levodopa and 3-O-methyldopa were measured by high-performance liquid chromatography for pharmacokinetic evaluation."( Comparative single- and multiple-dose pharmacokinetics of levodopa and 3-O-methyldopa following a new dual-release and a conventional slow-release formulation of levodopa and benserazide in healthy volunteers.
Crevoisier, C; Metzger, B; Monreal, A; Nilsen, T, 2003
)
0.32
" 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 validated method was applied in a pharmacokinetic study with a levodopa/benserazide tablet formulation in healthy volunteers."( Simultaneous quantitation of levodopa and 3-O-methyldopa in human plasma by HPLC-ESI-MS/MS: application for a pharmacokinetic study with a levodopa/benserazide formulation.
Bonfim, RR; Byrro, RM; Cardoso, FF; César, Ida C; da Silva, EP; Gomes, SA; Mundim, IM; Pianetti, GA; Teixeira, Lde S, 2011
)
0.37

Compound-Compound Interactions

Isradipine is superior to methyldopa and, whether as monotherapy or in combination with captopril, highly effective and well tolerated.

ExcerptReferenceRelevance
"The clinical actions of levodopa in Parkinsonism, given with and without an extracerebral decarboxylase in hibitor, L-alpha-methyldopahydrazine, were compared."( Idiopathic Parkinsonism treated with an extracerebral decarboxylase inhibitor in combination with levodopa.
Calne, DB; Gawler, J; Hilson, A; Pallis, CA; Petrie, A; Rao, S; Reid, JL; Thomas, PK; Vakil, SD, 1971
)
0.25
" These results indicate that isradipine is superior to methyldopa and, whether as monotherapy or in combination with captopril, highly effective and well tolerated in the treatment of mild-to-moderate hypertension."( A multicenter, double-blind, randomized, placebo-controlled study of isradipine and methyldopa as monotherapy or in combination with captopril in the treatment of hypertension. The LOMIR-MCT-IH Research Group.
Cristal, N; Yodfat, Y, 1993
)
0.29
"001) than patients treated with any of the monotherapies or with methyldopa in combination with captopril."( Quality of life in normotensives compared to hypertensive men treated with isradipine or methyldopa as monotherapy or in combination with captopril: the LOMIR-MCT-IL study.
Amir, M; Bar-On, D; Cristal, N; Yodfat, Y, 1996
)
0.29
"An HPLC method combined with second-order calibration based on alternating trilinear decomposition (ATLD) algorithm has been developed for the quantitative analysis of levodopa (LVD), carbidopa (CBD) and methyldopa (MTD) in human plasma samples."( Quantitative analysis of levodopa, carbidopa and methyldopa in human plasma samples using HPLC-DAD combined with second-order calibration based on alternating trilinear decomposition algorithm.
Fu, HY; Li, SF; Li, YN; Nie, JF; Wu, HL; Yu, RQ; Yu, YJ, 2010
)
0.36

Bioavailability

Absorption of methyldopa from the gastrointestinal tract is incomplete and variable. bioavailability after oral administration is about 25% (range 8 to 62%). Thus, the oral dose of POE was well absorbed and rapidly hydrolyzed to methylderopa.

ExcerptReferenceRelevance
" We have developed a high-pressure liquid chromatographic assay to determine the plasma-time concentrations of alpha-MD after intravenous administration of methyldopate and alpha-MD in the monkey in an effort to evaluate the bioavailability of alpha-MD and the extent of in vivo hydrolysis of the amino ester to the amino acid."( Metabolic disposition and cardiovascular effects of methyldopate in unanesthetized rhesus monkeys.
Castagnoli, N; Forsyth, RP; Marshall, KS; Melmon, KL; Rapoport, R; Walson, PD, 1975
)
0.25
" It is well absorbed orally."( [Long-range therapy of hypertension].
Radó, J; Szám, I; Takó, J, 1976
)
0.26
" Almost equivalent bioavailability (85-90%) of levodopa was demonstrated for the controlled-release formulations relative to that of conventional Madopar capsules."( Comparative multiple-dose pharmacokinetics of controlled-release levodopa products.
Collin, C; Eckernäs, SA; Grahnén, A; Ling-Andersson, A; Nilsson, M; Tiger, G, 1992
)
0.28
"4) is consistent with the incomplete oral bioavailability of this drug."( Concentration and pH dependency of alpha-methyldopa absorption in rat intestine.
Amidon, GL; Dressman, JB; Merfeld, AE, 1986
)
0.27
"Acylcarnitines were tested as potential absorption-enhancing agents for drugs that are poorly absorbed from the gastrointestinal tract."( Acylcarnitines: drug absorption-enhancing agents in the gastrointestinal tract.
Alexander, J; Engle, K; Fix, JA; Gardner, CR; Leppert, PS; Porter, PA; Selk, SJ, 1986
)
0.27
" Thus, although absorption of alpha-methyldopa is more efficient at lower concentrations, bioavailability may not be substantially enhanced due to increased sulphation in the gut wall."( The effect of pH and concentration on alpha-methyldopa absorption in man.
Admidon, GL; Cortese, MA; Dressman, JB; Merfeld, AE; Mlodozeniec, AR; Rhodes, JB, 1986
)
0.27
" 163, administered as their DL-racemic mixtures, produced increases in the t1/2 and bioavailability of co-administered L-DOPA comparable to that produced by a 10-fold larger dose of carbidopa administered as the active L-enantiomer; increasing the dose of MDL 72."( A comparison of the effects of reversible and irreversible inhibitors of aromatic L-amino acid decarboxylase on the half-life and other pharmacokinetic parameters of oral L-3,4-dihydroxyphenylalanine.
Haegele, KD; Huebert, ND; Palfreyman, MG,
)
0.13
" Thus, the oral dose of POE was well absorbed and rapidly hydrolyzed to methyldopa."( Metabolism of methyldopa in man after oral administration of the pivaloyloxyethyl ester.
Dobrinska, MR; Dollery, CT; Duncan, CA; Gomez, HJ; Leidy, HL; Ramjit, HG; Vickers, S; Vincek, WC,
)
0.13
" alpha MD ethyl ester administration resulted in higher alpha MD levels in CSF as compared with alpha MD administration, suggesting a higher bioavailability of the ethyl ester vs the free acid."( Determination of alphamethyldopa, dihydroxyphenylacetic acid and 5-hydroxyindolacetic acid in the cerebrospinal fluid of the rat: kinetic study.
Elghozi, JL; Laude, D; Meyer, P; Mignot, E, 1983
)
0.27
" Bioavailability studies in dogs show that the esters, particularly the 5-methyl derivative, yield significant plasma levels of methyldopa."( 3-Hydroxy-alpha-methyltyrosine progenitors: synthesis and evaluation of some (2-oxo-1,3-dioxol-4-yl)methyl esters.
Cochran, DW; Dobrinska, MR; Gaul, SL; Halczenko, W; Saari, WS; Sweet, CS; Titus, DC; Vincek, WC, 1984
)
0.27
"The pivaloyloxyethyl ester of methyldopa is an antihypertensive prodrug possessing improved bioavailability properties over methyldopa."( Sensitive high-performance liquid chromatographic assay using electrochemical detection for a novel prodrug ester of methyldopa, pivaloyloxyethyl 3-(3,4-dihydroxyphenyl)-2-methylalaninate, in plasma and urine.
Dobrinska, MR; Leidy, HL; Musson, DG; Vickers, S; Vincek, WC, 1984
)
0.27
" These findings confirm the importance of using indices other than drug plasma concentrations in the assessment of bioavailability in disease states."( The absorption and conjugation of methyldopa in patients with coeliac and Crohn's diseases during treatment.
George, CF; Higgins, V; Powers, K; Renwick, AG; Smith, CL, 1983
)
0.27
"Absorption of methyldopa from the gastrointestinal tract is incomplete and variable; bioavailability after oral administration is about 25% (range 8 to 62%)."( Clinical pharmacokinetics of methyldopa.
Hansen, T; Myhre, E; Rugstad, HE,
)
0.13
" The absolute bioavailability of the drug was 42 +/- 16%."( Pharmacokinetics and presystemic gut metabolism of methyldopa in healthy human subjects.
Campbell, NR; Robertson, S; Skerjanec, A; Tam, YK, 1995
)
0.29
"In a single dose, randomized, cross-over study, with one week of wash-out period, the relative bioavailability of Dopegyt tablets containing 250 mg alpha-methyldopa (AMD) and Presinol film tablets with identical active ingredient content was examined in 24 healthy volunteers."( Comparative bioavailability of alpha-methyldopa normal and film tablet formulations after single oral administration in healthy volunteers.
Ary, K; Drabant, S; Gachályi, B; Grézal, GY; Klebovich, I; Renczes, G; Róna, K,
)
0.13
" The relative bioavailability (Madopar DR vs."( Comparative single- and multiple-dose pharmacokinetics of levodopa and 3-O-methyldopa following a new dual-release and a conventional slow-release formulation of levodopa and benserazide in healthy volunteers.
Crevoisier, C; Metzger, B; Monreal, A; Nilsen, T, 2003
)
0.32
"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
"The purpose of the present study was to compare the bioavailability of a new methyldopa (CAS 555-30-6) tablet formulation with that of a reference formulation in 12 healthy male subjects using a modified HPLC method."( Single dose bioequivalence study of alpha-methyldopa tablet formulations using a modified HPLC method.
Ansarin, M; Hallaj-Nezhadi, S; Nemati, M; Valizadeh, H; Zakeri-Milani, P, 2010
)
0.36
"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
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

The dose-response relationship for the different doses of alpha-methyldopa in combination with chlorpromazine, suggested an optimal response to 300 mg chlor Promazine--500 mg alpha-MethyldOPA. Pretreatment with the opiate receptor antagonist naltrexone resulted in a parallel shift to the right of the dose- response curve for alpha- methyldopamine.

ExcerptRelevanceReference
" A connection between duration and dosage of the treatment with alpha-methyldopa and these hepatological findings could not be ascertained statistically."( [The problems of adverse effects to the liver of alpha-methyldopa].
Zenos, A, 1977
)
0.26
" Half the patients responded will to low dosage (oxprenolol less than or equal to 320 mg, methyldopa less than or equal to 1 g, a day) and 9 of 11 such patients responded satisfactorily to each drug."( Comparison of oxprenolol and methyldopa in hypertension. A within-patient double-blind trial.
Barritt, DW; Heaton, S; Marshall, AJ, 1976
)
0.26
" 4 Dosage varied; average 889 mg/d, range 75-3,200 mg."( Labetalol in long-term treatment of hypertension.
Boakes, AJ; Prichard, BN, 1976
)
0.26
" The first dose was given 1 h before rising, and the daily dosage was progressively increased."( Dihydroergotamine: an effective treatment for postural hypotension due to antihypertensive drugs (ganglion-blocking agents excepted).
Conté, JJ; Fournié, GJ; Maurette, MH, 1976
)
0.26
" Dose-response relationships showed the same correlations and lack of correlations, respectively."( On the role of alpha-methyldopamine in the antihypertensive effect of alpha-methyldopa.
Hedwal, PR; Maître, L; Waldmeier, P, 1975
)
0.25
" Advanced age modifies the approach to treatment; the choice of drugs and the dosage must be adjusted accordingly."( Drug therapy for cardiovascular disease in the aged.
Kennedy, RD, 1975
)
0.25
"Pharmacokinetic methods that have been used to improve antihypertensive drug therapy, including antihypertensive dosage regimens, are reviewed."( Using pharmacokinetics in drug therapy. V: Contributions to developing dosage regimens for antihypertensive drugs.
Schumacher, GE, 1979
)
0.26
" The simple dosage regime, combined with proven effectiveness and a relative lack of side-effects makes atenolol a useful treatment for the hypertensive patient."( Multicentre general practitioner assessment of 'Tenormin' and methyldopa.
Mason, B; Sleigh, R; Tweed, JA, 1979
)
0.26
"7 years) with severe essential hypertension (n = 21) and renovascular hypertension (n = 1) were treated with a mean daily dosage of 16."( [Minoxidil in treatment resistant hypertension].
Furrer, J; Nussberger, J; Reuteler, H; Siegenthaler, W; Studer, A; Tenschert, W; Vetter, W, 1979
)
0.26
"The stability of liquid dosage forms of ethacrynic acid (1 mg/ml), indomethacin (2 mg/ml), methyldopate hydrochloride (25 mg/ml), prednisone (0."( Stability of pediatric liquid dosage forms of ethacrynic acid, indomethacin, methyldopate hydrochloride, prednisone and spironolactone.
Das Gupta, V; Ghanekar, AG; Gibbs, CW, 1978
)
0.26
" Paired ion chromatography also was tried successfully for the quantitative determinations of isoproterenol, levodopa, methyldopa, and phenylephrine in some dosage forms."( Applications of paired ion high-pressure liquid chromatography to catecholamines and phenylephrine.
Das Gupta, D; Ghanekar, AG, 1978
)
0.26
" Although the three treatment regimens were similar with respect to safety and efficacy, the reserpine-hydroflumethiazide combination offers the advantages of more convenient dosage at lower cost."( Step 2 regimens in hypertension. An assessment.
Berry, C; Finnerty, FA; Gyftopoulos, A; McKenney, A, 1979
)
0.26
" The dose-response relationship for the different doses of alpha-methyldopa in combination with chlorpromazine, suggested an optimal response to 300 mg chlorpromazine--500 mg alpha-methyldopa."( Alpha-methyldopa-chlorpromazine combination in schizophrenic patients.
Annable, L; Chouinard, G, 1976
)
0.26
"Where practicable, all subjects found with onset-phase-four blood pressure of 90 mmHg or more after referral were allocated, on a random basis, to alternative antihypertensive regimes at a dosage related to response."( An approach to realistic evaluation of antihypertensive regimes.
Akinkugbe, OO; Basile, U; Carlisle, R; Solagbade, ME, 1977
)
0.26
" Side effects (hallucinations, confusion, dyskinesias) were frequent, but were usually reversible by lowering the dosage of levodopa or the accompanying anticholinergic medication."( Piribedil: its synergistic effect in multidrug regimens for parkinsonism.
Feigenson, JS; McDowell, FH; Sweet, RD, 1976
)
0.26
" Systemic administration of alpha-methyldopa to rats for 15 days shifted the log dose-response curves for all three catecholamines, but not vasopressin or potassium chloride, to the right of all three blood vessel types; the maximal contractile responses to these amines were, however, not affected by chronic treatment with alpha-methyldopa."( Pharmacological effects of alpha-methyldopa, alpha-methylnorepinephrine, and octopamine on rat arteriolar, arterial, and terminal vascular smooth.
Altura, BM, 1975
)
0.25
" No foreign related amino acid impurities were detected in any of the three commercial dosage forms examined."( Specific quantitative gas-liquid chromatographic analysis of methyldopa and some foreign related amino acids in raw material and commercial tablets.
Lawrence, RC; Watson, JR, 1975
)
0.25
" The drugs could be given in a twice-daily dosage and had a much higher degree of patient acceptance."( Oxprenolol and hydrallazine in the treatment of hypertension.
Freeman, JW; Knight, LW, 1975
)
0.25
" For the inhibition of the hypotensive action of clonidine by protriptyline a parallel shift of the dose-response curve was obtained, indicating the possibility of a competitive antagonism."( Interaction between centrally acting hypotensive drugs and tricyclic antidepressants.
van Zwieten, PA, 1975
)
0.25
", were much higher in chronically dosed animals."( Effects of chronic oral administration on the disposition of laevodopa and its major metabolites in the plasma of the rat.
Cheng, LK; Fung, HL, 1975
)
0.25
" dosage schedule."( Comparative multiple-dose pharmacokinetics of controlled-release levodopa products.
Collin, C; Eckernäs, SA; Grahnén, A; Ling-Andersson, A; Nilsson, M; Tiger, G, 1992
)
0.28
" The principal disadvantages of this class of medications are an overlap between the therapeutic dosage and that producing sedation and dry mouth and the potential to cause the discontinuation syndrome and sexual dysfunction."( Use of centrally acting sympatholytic agents in the management of hypertension.
Epstein, M; Oster, JR, 1991
)
0.28
" Continued dosage impairs psychometric performance, but practice effect is a major confounder."( Effects of methyldopa on psychometric performance.
Errichetti, A; Hoch, K; Johnson, B; Johnson, J, 1990
)
0.28
" From dose-response curves, near-maximal intracisternal (i."( Differential blood pressure responses to intracisternal clonidine, alpha-methyldopa, and 6-hydroxydopamine in conscious normotensive and spontaneously hypertensive rats.
de Jong, W; Head, GA,
)
0.13
" The twice daily dosage schedule caused trough blood pressure control with both drugs."( Evaluation of a new antihypertensive agent ketanserin versus methyldopa in the treatment of essential hypertension in older patients: an international multicenter trial.
Alcocer, L; Copertari, P; Feruglio, F; Landi, E; Lopes, M; San Martin, C; Zin, C, 1987
)
0.27
" For blood pressure and heart rate, pretreatment with a midportion beta-endorphin antiserum resulted in a parallel shift to the right of the dose-response curve for alpha-methyldopa."( Possible involvement of beta endorphin(1-31) and dynorphin(1-13) in the central hypotensive mechanism of action of alpha methyldopa.
de Jong, W; van Giersbergen, PL; Wiegant, VM, 1989
)
0.28
" The data also demonstrated effectiveness with aqueous and solid dosage forms (Witepsol H-15 suppositories)."( Acylcarnitines: drug absorption-enhancing agents in the gastrointestinal tract.
Alexander, J; Engle, K; Fix, JA; Gardner, CR; Leppert, PS; Porter, PA; Selk, SJ, 1986
)
0.27
" Pretreatment with the opiate receptor antagonist naltrexone resulted in a parallel shift to the right of the dose-response curve for alpha-methyldopa, both for blood pressure and heart rate."( Antagonism by naltrexone of the hypotension and bradycardia induced by alpha-methyldopa in conscious normotensive rats.
de Jong, W; van Giersbergen, PL, 1988
)
0.27
"02; 2--A more frequent adjustment of daily dosage with MD (n = 15) than with ACE (n = 10) or LAB (n = 7); 3--The absence of any significant difference for uricemia level, platelet counts, foetal cardiac rythm, and occurrence of pre-eclampsia (MD = 4; ACE = 3; LAB = 4; 4--An equivalent birth-weight (MD = 3110 +/- 628 g; ACE = 3115 +/- 645."( [Randomized, comparative study on the treatment of moderate arterial hypertension during pregnancy: methyldopa, acebutolol, labetalol].
Blazquez, G; Gérard, J; Lardoux, H; Leperlier, E, 1988
)
0.27
" Dosage was titrated until blood pressures were normalized (diastolic blood pressure (DBP) less than or equal to 95 mmHg) (1 mmHg = 133."( A novel therapeutic approach for reversal of left ventricular hypertrophy and blood pressure control in hypertensive patients treated with alpha-methyldopa or propranolol.
Fernandez, PG; Kim, BK; Lee, CC; Snedden, W, 1985
)
0.27
" The method has been adopted official first action for determination of the active ingredients in levodopa tablets and capsules and in levodopa-carbidopa tablets and for content uniformity testing in the combination dosage form."( Liquid chromatographic determination of levodopa and levodopa-carbidopa in solid dosage forms: collaborative study.
Ting, S,
)
0.13
" It is concluded that alpha-methyldopa is efficacious against climacteric hot flushes when given as single evening doses, but further study is required to answer whether this dosage is as effective as a twice daily regimen."( alpha-Methyldopa for climacteric hot flushes. A double-blind, randomized, cross-over study.
Andersen, O; Engebretsen, T; Orbo, A; Solberg, VM, 1986
)
0.27
" Decreased fertility was seen in males dosed with 200 or 400 mg/kg methyldopa."( Reproductive toxicology of methyldopa in male F344/N rats.
Chapin, RE; Dunnick, JK; Hall, LB; Harris, MW; Lamb, JC, 1986
)
0.27
"To assess the problem of alpha-methyldopa dosing in lactating mothers with hypertension, we studied three breast-feeding women to determine simultaneous plasma and breast milk concentrations of alpha-methyldopa after a 500 mg oral dose while receiving continuous therapy."( Alpha-methyldopa disposition in mothers with hypertension and in their breast-fed infants.
Andreoli, JW; Cohn, RD; White, WB, 1985
)
0.27
"1 N HCl, but not the same drug dosage at neutral pH or saline, resulted in reduction of voluntary drinking of ethanol by the male rat."( Neurotoxicological analyses of voluntary alcohol drinking by the rat.
Messiha, FS,
)
0.13
" Determinations on dosage forms of the drugs, using PDAC and PDAB reagents, agreed well with results of determinations by official pharmacopoeial methods."( Colorimetric determination of sympathomimetic amines methyldopa and noradrenaline.
Abou Ouf, A; Salem, FB; Walash, MI,
)
0.13
" alpha-Methyldopa and clonidine produced the same hypotensive response at 6 and 8 h after dosing with a similar fall in plasma noradrenaline levels at these times."( The plasma noradrenaline and growth hormone response to alpha-methyldopa and clonidine in hypertensive subjects.
Adams, EF; Brown, MJ; Dollery, CT; Struthers, AD, 1985
)
0.27
" Pressor dose-response relationships for noradrenaline were the same before and after L-DOPA, as well as in cats pretreated with L-DOPA for 4 days."( On the mechanism of L-dopa-induced postural hypotension in the cat.
Dhasmana, KM; Spilker, BA, 1973
)
0.25
" The rise in brain histamine after dosage with histidine persisted for several hours, depending on the dose; with 500 mg/kg, the rise was virtually unchanged after 16 hours."( Concentration of histamine in different parts of the brain and hypophysis of rabbit: effect of treatment with histidine, certain other amino acids and histamine.
Abou, YZ; Adam, HM; Stephen, WR, 1973
)
0.25
"The requirement for insulin decreased in both patients during the period of renal insufficiency and increased following transplantation; this seemed to be related to the large dose of steroids given because now that a maintenance level of steroids has been established, both patients require the same dosage of insulin as they did before the onset of renal insufficiency."( Treatment of renal failure from diabetic nephropathy with cadaveric homograft.
Beaudry, C; Laplate, L, 1973
)
0.25
"The blood pressure and pulse rate have been compared in a 'double blind, cross over' study involving twenty patients with idiopathic Parkinsonism receiving maximum tolerated dosage of levodopa with and without an extracerebral decarboxylase inhibitor, L-alpha-methyldopahydrazine."( Action of L- -methyldopa-hydrazine on the blood pressure of patients receiving levodopa.
Calne, DB; Petrie, A; Rao, S; Reid, JL; Vakil, SD, 1972
)
0.25
"Sensitivity to propranolol varies widely, and dosage should be increased gradually."( Treatment of hypertension with propranolol.
Gillam, PM; Prichard, BN, 1969
)
0.25
" In patients who respond to modest doses of pindolol, twice or even once daily dosing is often adequate."( Pindolol: a review of its pharmacology, pharmacokinetics, clinical uses, and adverse effects.
Golightly, LK,
)
0.13
" A dosage of 100mg twice daily will often be adequate to control mild hypertension and the use of even lower doses has been reported."( Combined alpha- and beta-receptor inhibition in the treatment of hypertension.
Prichard, BN, 1984
)
0.27
" Dosage was titrated until normotension was attained and patients were then maintained on this treatment for a year."( The correlation of changes in systolic blood pressure with regional anatomical regression of hypertensive left ventricular hypertrophy in patients on chronic antihypertensive therapy (greater than 1 year): alpha-methyldopa compared to propranolol.
Fernandez, PG; Furlong, L; Gill, V; Kim, BK; Ko, P; Lewis, H; McDonald, J; McManamon, P; Nolan, R; Reichek, N, 1984
)
0.27
" The clinical appearance of oral ulcerations coincides with increased dosage of the drug."( Oral drug reaction to methyldopa. Report of a case.
Williams, BG, 1983
)
0.27
" All groups had mean diastolic pressure controlled at or below the 90 mmHg criterion during the period of constant methyldopa dosage for those patients who required Step 2 therapy."( Indapamide in the stepped-care treatment of obese hypertensive patients.
Godfrey, JC; Neiss, ES; Noble, RE; Vukovich, RA; Webb, EL; Zisblatt, M, 1983
)
0.27
" Recoveries from commercial dosage forms ranged from 99."( Liquid chromatographic determination of methyldopa and methyldopa-thiazide combinations in dosage forms.
Ting, S, 1983
)
0.27
" Prior to study, 2 hours post dosing and coincident with immediate pre-exercise on treadmill, at graded increases of exercise and 2 hours post exercise (approximately 4 hours post dosing), blood was sampled for potassium, renin concentration, aldosterone and catecholamines."( Potassium disposition and neuroendocrine effects of propranolol, methyldopa and clonidine during dynamic exercise.
Affrime, MB; Falkner, B; Hakki, H; Lowenthal, DT; Rosenthal, L; Saris, S, 1982
)
0.26
" Before the study, 2 hr after dosing and coincident with immediate preexercise on treadmill (at graded increases of exercise), and 2 hr after exercise, blood was sampled for determination of potassium, renin, aldosterone, and catecholamine levels."( Biochemical and dynamic responses to single and repeated doses of methyldopa and propranolol during dynamic physical activity.
Affrime, MB; Falkner, B; Gould, AB; Lowenthal, DT; Rosenthal, L; Saris, S, 1982
)
0.26
" The mean daily dosage was 1359 mg."( An intra-arterial profile of methyldopa.
Cashman, PM; Gould, BA; Hornung, RS; Kieso, HA; Raftery, EB, 1983
)
0.27
" As the reason for the weak effectiveness of alpha-methyldopa on the incidence of AIHA, it might be considered that the dosage employed was not sufficiently high enough and/or it may be due to the species difference between man and animals."( Influence of carbidopa, an aromatic amino acid decarboxylase inhibitor, on the development of autoimmune hemolytic anemia in NZB mice.
Kemi, M; Kondo, M; Maki, E; Tanabe, K, 1983
)
0.27
" Patients were started on either 100 mg labetalol or 250 mg alpha-methyldopa 3-times daily and, if necessary, the dosage adjusted by standard increments every 2 weeks over a period of a month until satisfactory control was achieved."( A controlled comparison of the antihypertensive effects of labetalol and alpha-methyldopa.
Al-Damluji, SF; Al-Khalidi, A; Shaarbaf, H; Tawfiq, NH, 1982
)
0.26
" Pindolol and propranolol lowered PRA comparably at equivalent dosages, although this effect was not consistently observed in all studies or at all dosage levels."( Pindolol: effects on blood pressure and plasma renin activity.
Bennett, CM; Glassock, RJ; Gonasun, L; Hamilton, B; Kirkendall, W; Maxwell, M; Weitzman, RE; Winer, N, 1982
)
0.26
" 4 The results suggest that the duration of antihypertensive effect of methyldopa is long enough to permit twice daily dosing, but that single daily dosing cannot be recommended for most patients."( Duration of effect of single daily dose methyldopa therapy.
Dollery, CT; Orozco-Gonzalez, M; Polak, G; Wright, JM, 1982
)
0.26
" These findings show that atenolol at the 100-mg daily dose is as effective as the full dosage of methyldopa and in addition shows better tolerance, a simpler therapeutic scheme, and less incidence of side effects."( Comparison of antihypertensive activity of atenolol and methyldopa at rest and during exercise.
Ambrosioni, E; Costa, FV; Magelli, C; Magnani, B; Malini, PL, 1981
)
0.26
" The age, degree of renal impairment, plasma renin activity, and number and dosage of antihypertensive medicines did not account for these differences in NE."( Effect of antihypertensive therapy on plasma catecholamines in renal failure patients.
Anderson, S; Cronin, R; Henrich, WL; Mitchell, H; Pettinger, WA, 1981
)
0.26
"Carbon tetrachloride induces diffuse fatty degeneration and centrilobular necrosis in the liver and the severity of liver injury is roughly proportional to the dosage administered."( [Toxic cirrhosis].
Kawasaki, H; Murawaki, Y; Yamada, S; Yamamoto, T, 1994
)
0.29
" The proposed methods were successfully applied to the assay of LD, MD, and DP in various dosage forms."( Spectrophotometric investigations of the assay of physiologically active catecholamines in pharmaceutical formulations.
Keshavayya, J; Melwanki, MB; Nagaralli, BS; Ramesh, KC; Seetharamappa, J,
)
0.13
" Depending on the intended indication and dosing regimen, PPL can delay or stop development of a compound in the drug discovery process."( Evaluation of a published in silico model and construction of a novel Bayesian model for predicting phospholipidosis inducing potential.
Gehlhaar, D; Greene, N; Johnson, TO; Pelletier, DJ; Tilloy-Ellul, A,
)
0.13
" Nifedipine dosage was based on the value of CYP3A4 gene expression."( [Methyldopa-induced acute reactive hepatitis in pregnancy, drug-metabolizing capacity of the liver].
Monostory, K; Ozsvár, Z; Solymossi, Z, 2010
)
0.36
" We now report on the choice of dopa decarboxylase inhibitors, dose and the time of dosing relationships of carbidopa, benserazide and L-alpha-methyl dopa (L-AMD) in potentiating the effects of L-DOPA in the 1-methyl-4-phenyl-1,2,3,6 tetrahydropyridine (MPTP)-treated common marmoset."( The timing of administration, dose dependence and efficacy of dopa decarboxylase inhibitors on the reversal of motor disability produced by L-DOPA in the MPTP-treated common marmoset.
Fisher, R; Jackson, MJ; Jenner, P; Rose, S; Tayarani-Binazir, KA; Zoubiane, G, 2010
)
0.36
" We proposed a systematic classification scheme using FDA-approved drug labeling to assess the DILI potential of drugs, which yielded a benchmark dataset with 287 drugs representing a wide range of therapeutic categories and daily dosage amounts."( FDA-approved drug labeling for the study of drug-induced liver injury.
Chen, M; Fang, H; Liu, Z; Shi, Q; Tong, W; Vijay, V, 2011
)
0.37
" Physicians managing hypertensive patients should pay attention not only to adequate dosing and appropriate combination of drugs but also to health education and patient counselling."( Drug utilization and blood pressure control in a population where antihypertensives are given free: effect of policy change.
Adedapo, AD; Adeleke, S; Okechukwu, R; Sikuade, O, 2012
)
0.38
" Aiming for evidence-based and personalized dosing of antihypertensive medication in the future, further studies on the relationship of both PK and pharmacodynamics (including the optimal blood pressure targeting) during pregnancy and pregnancy-related pathology are urgently needed to prevent undertreatment, overtreatment, and side effects."( Pharmacokinetics of the most commonly used antihypertensive drugs throughout pregnancy methyldopa, labetalol, and nifedipine: a systematic review.
Allegaert, K; Flint, RB; Mian, P; Schoenmakers, S; van de Vusse, D; Versmissen, J; Visser, W, 2022
)
0.72
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (5)

RoleDescription
haptenAny substance capable of eliciting an immune response only when attached to a large carrier such as a protein. Examples include dinitrophenols; oligosaccharides; peptides; and heavy metals.
antihypertensive agentAny drug used in the treatment of acute or chronic vascular hypertension regardless of pharmacological mechanism.
alpha-adrenergic agonistAn agent that selectively binds to and activates alpha-adrenergic receptors.
peripheral nervous system drugA drug that acts principally at one or more sites within the peripheral neuroeffector systems, the autonomic system, and motor nerve-skeletal system.
sympatholytic agentAny compound which inhibits the postganglionic functioning of the sympathetic nervous system (SNS).
[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
L-tyrosine derivativeA proteinogenic amino acid derivative resulting from reaction of L-tyrosine at the amino group or the carboxy group, or from the replacement of any hydrogen of L-tyrosine by a heteroatom.
non-proteinogenic L-alpha-amino acidAny L-alpha-amino acid which is not a member of the group of 23 proteinogenic amino acids.
[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 (94)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency3.55010.003245.467312,589.2998AID1705; AID2517
Chain A, TYROSYL-DNA PHOSPHODIESTERASEHomo sapiens (human)Potency0.64780.004023.8416100.0000AID485290
Chain A, Beta-lactamaseEscherichia coli K-12Potency53.80830.044717.8581100.0000AID485294; AID485341
Chain A, Putative fructose-1,6-bisphosphate aldolaseGiardia intestinalisPotency14.34210.140911.194039.8107AID2451
Chain A, HADH2 proteinHomo sapiens (human)Potency0.12590.025120.237639.8107AID886
Chain B, HADH2 proteinHomo sapiens (human)Potency0.12590.025120.237639.8107AID886
Chain A, JmjC domain-containing histone demethylation protein 3AHomo sapiens (human)Potency19.95260.631035.7641100.0000AID504339
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency9.91500.177814.390939.8107AID2147
Chain A, ATP-DEPENDENT DNA HELICASE Q1Homo sapiens (human)Potency2.39980.125919.1169125.8920AID2549; AID2708
endonuclease IVEscherichia coliPotency31.62280.707912.432431.6228AID1708
acetylcholinesteraseHomo sapiens (human)Potency75.86350.002541.796015,848.9004AID1347395; AID1347398
thioredoxin reductaseRattus norvegicus (Norway rat)Potency10.43840.100020.879379.4328AID488773; AID588453
15-lipoxygenase, partialHomo sapiens (human)Potency1.25890.012610.691788.5700AID887
phosphopantetheinyl transferaseBacillus subtilisPotency37.66390.141337.9142100.0000AID1490; AID2701
GLS proteinHomo sapiens (human)Potency8.64380.35487.935539.8107AID624146; AID624170
TDP1 proteinHomo sapiens (human)Potency28.42450.000811.382244.6684AID686978; AID686979
GLI family zinc finger 3Homo sapiens (human)Potency43.71300.000714.592883.7951AID1259369; AID1259392
Microtubule-associated protein tauHomo sapiens (human)Potency11.68520.180013.557439.8107AID1460; AID1468
thioredoxin glutathione reductaseSchistosoma mansoniPotency22.38720.100022.9075100.0000AID485364
Smad3Homo sapiens (human)Potency3.98110.00527.809829.0929AID588855
apical membrane antigen 1, AMA1Plasmodium falciparum 3D7Potency11.22020.707912.194339.8107AID720542
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency15.26450.011212.4002100.0000AID1030
hypothetical protein, conservedTrypanosoma bruceiPotency13.45910.223911.245135.4813AID624147
regulator of G-protein signaling 4Homo sapiens (human)Potency26.67950.531815.435837.6858AID504845
estrogen nuclear receptor alphaHomo sapiens (human)Potency0.61570.000229.305416,493.5996AID743079
bromodomain adjacent to zinc finger domain 2BHomo sapiens (human)Potency15.84890.707936.904389.1251AID504333
arylsulfatase AHomo sapiens (human)Potency37.93301.069113.955137.9330AID720538
pyruvate kinaseLeishmania mexicana mexicanaPotency0.79430.398113.744731.6228AID945; AID959
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency1.45700.035520.977089.1251AID504332
Histone H2A.xCricetulus griseus (Chinese hamster)Potency61.25060.039147.5451146.8240AID1224845; AID1224896
Bloom syndrome protein isoform 1Homo sapiens (human)Potency8.29300.540617.639296.1227AID2364; AID2528
lysosomal alpha-glucosidase preproproteinHomo sapiens (human)Potency3.54810.036619.637650.1187AID2100
peripheral myelin protein 22 isoform 1Homo sapiens (human)Potency84.921423.934123.934123.9341AID1967
15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1Homo sapiens (human)Potency28.79680.001815.663839.8107AID894
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency50.11870.354828.065989.1251AID504847
chromobox protein homolog 1Homo sapiens (human)Potency15.03630.006026.168889.1251AID488953; AID540317
importin subunit beta-1 isoform 1Homo sapiens (human)Potency112.20205.804836.130665.1308AID540263
DNA polymerase betaHomo sapiens (human)Potency1.26730.022421.010289.1251AID485314
flap endonuclease 1Homo sapiens (human)Potency33.40200.133725.412989.1251AID488816; AID588795; AID720498
ubiquitin carboxyl-terminal hydrolase 2 isoform aHomo sapiens (human)Potency22.38720.65619.452025.1189AID463254
serine/threonine-protein kinase mTOR isoform 1Homo sapiens (human)Potency23.00140.00378.618923.2809AID2660; AID2666; AID2667; AID2668
snurportin-1Homo sapiens (human)Potency112.20205.804836.130665.1308AID540263
peptidyl-prolyl cis-trans isomerase NIMA-interacting 1Homo sapiens (human)Potency50.11870.425612.059128.1838AID504891
DNA polymerase eta isoform 1Homo sapiens (human)Potency3.16230.100028.9256213.3130AID588591
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency9.95650.050127.073689.1251AID588590
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency35.48130.00798.23321,122.0200AID2546; AID2551
gemininHomo sapiens (human)Potency2.70560.004611.374133.4983AID624296; AID624297
DNA polymerase kappa isoform 1Homo sapiens (human)Potency5.04280.031622.3146100.0000AID588579
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency15.84890.031610.279239.8107AID884; AID885
M-phase phosphoprotein 8Homo sapiens (human)Potency23.27860.177824.735279.4328AID488949
muscleblind-like protein 1 isoform 1Homo sapiens (human)Potency50.11870.00419.962528.1838AID2675
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency11.03430.251215.843239.8107AID504327
lethal factor (plasmid)Bacillus anthracis str. A2012Potency31.62280.020010.786931.6228AID912
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Rap guanine nucleotide exchange factor 3Homo sapiens (human)Potency10.00006.309660.2008112.2020AID720709
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
D(1A) dopamine receptorSus scrofa (pig)Potency23.28090.00378.108123.2809AID2667
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
GABA theta subunitRattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Ataxin-2Homo sapiens (human)Potency22.38720.011912.222168.7989AID588378
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
phosphoglycerate kinaseTrypanosoma brucei brucei TREU927Potency2.13310.07578.474229.0628AID504547
2,3-bisphosphoglycerate-independent phosphoglycerate mutaseLeishmania major strain FriedlinPotency37.93307.568615.230621.3313AID504548
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency20.59200.060110.745337.9330AID485367; AID485368; AID504636; AID504637
acetylcholinesteraseHomo sapiens (human)Potency43.64860.002541.796015,848.9004AID1347398
phosphopantetheinyl transferaseBacillus subtilisPotency22.38720.141337.9142100.0000AID1490
RAR-related orphan receptor gammaMus musculus (house mouse)Potency7.41460.006038.004119,952.5996AID1159521; AID1159523
TDP1 proteinHomo sapiens (human)Potency29.85540.000811.382244.6684AID686978
GLI family zinc finger 3Homo sapiens (human)Potency49.61460.000714.592883.7951AID1259369; AID1259392
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency4.36490.01237.983543.2770AID1645841
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency7.56240.000214.376460.0339AID720691
estrogen nuclear receptor alphaHomo sapiens (human)Potency4.35400.000229.305416,493.5996AID743075
cytochrome P450 2D6Homo sapiens (human)Potency24.54540.00108.379861.1304AID1645840
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency24.48420.023723.228263.5986AID743223
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency0.79430.035520.977089.1251AID504332
thyroid stimulating hormone receptorHomo sapiens (human)Potency68.58960.001628.015177.1139AID1259385
v-jun sarcoma virus 17 oncogene homolog (avian)Homo sapiens (human)Potency41.10420.057821.109761.2679AID1159528
Histone H2A.xCricetulus griseus (Chinese hamster)Potency42.83350.039147.5451146.8240AID1224845
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency89.12510.354828.065989.1251AID504847
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency68.38040.000323.4451159.6830AID743065; AID743067
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency38.21960.000627.21521,122.0200AID651741; AID743219
DNA polymerase kappa isoform 1Homo sapiens (human)Potency3.35870.031622.3146100.0000AID588579
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency11.22020.251215.843239.8107AID504327
lamin isoform A-delta10Homo sapiens (human)Potency35.48130.891312.067628.1838AID1487
[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)
estrogen receptor beta isoform 1Homo sapiens (human)IC50 (µMol)50.00001.91098.316518.7976AID733
Bile salt export pumpRattus norvegicus (Norway rat)IC50 (µMol)1,000.00000.40002.75008.6000AID1209456
Bile salt export pumpHomo sapiens (human)IC50 (µMol)1,000.00000.11007.190310.0000AID1209455; AID1449628
Epidermal growth factor receptorHomo sapiens (human)IC50 (µMol)5.22800.00000.536910.0000AID625184
Tyrosine-protein kinase FynHomo sapiens (human)IC50 (µMol)5.17600.00021.67898.6800AID625185
Polyunsaturated fatty acid lipoxygenase ALOX15Oryctolagus cuniculus (rabbit)IC50 (µMol)2.12600.11003.26419.0330AID625146
Cystathionine gamma-lyaseHomo sapiens (human)IC50 (µMol)3,000.00000.57002.86098.0000AID1800301
Solute carrier family 15 member 1Homo sapiens (human)IC50 (µMol)151,600.00000.18000.19000.2000AID681608
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Caspase 6, apoptosis-related cysteine peptidaseHomo sapiens (human)AC5039.23000.063611.235844.9700AID720632
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (203)

Processvia Protein(s)Taxonomy
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)
angiogenesisRap guanine nucleotide exchange factor 3Homo sapiens (human)
adaptive immune responseRap guanine nucleotide exchange factor 3Homo sapiens (human)
signal transductionRap guanine nucleotide exchange factor 3Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayRap guanine nucleotide exchange factor 3Homo sapiens (human)
associative learningRap guanine nucleotide exchange factor 3Homo sapiens (human)
Rap protein signal transductionRap guanine nucleotide exchange factor 3Homo sapiens (human)
regulation of actin cytoskeleton organizationRap guanine nucleotide exchange factor 3Homo sapiens (human)
negative regulation of syncytium formation by plasma membrane fusionRap guanine nucleotide exchange factor 3Homo sapiens (human)
intracellular signal transductionRap guanine nucleotide exchange factor 3Homo sapiens (human)
positive regulation of GTPase activityRap guanine nucleotide exchange factor 3Homo sapiens (human)
regulation of angiogenesisRap guanine nucleotide exchange factor 3Homo sapiens (human)
positive regulation of angiogenesisRap guanine nucleotide exchange factor 3Homo sapiens (human)
positive regulation of protein export from nucleusRap guanine nucleotide exchange factor 3Homo sapiens (human)
positive regulation of stress fiber assemblyRap guanine nucleotide exchange factor 3Homo sapiens (human)
regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionRap guanine nucleotide exchange factor 3Homo sapiens (human)
positive regulation of syncytium formation by plasma membrane fusionRap guanine nucleotide exchange factor 3Homo sapiens (human)
establishment of endothelial barrierRap guanine nucleotide exchange factor 3Homo sapiens (human)
cellular response to cAMPRap guanine nucleotide exchange factor 3Homo sapiens (human)
Ras protein signal transductionRap guanine nucleotide exchange factor 3Homo sapiens (human)
regulation of insulin secretionRap guanine nucleotide exchange factor 3Homo sapiens (human)
cell surface receptor signaling pathwayEpidermal growth factor receptorHomo sapiens (human)
epidermal growth factor receptor signaling pathwayEpidermal growth factor receptorHomo sapiens (human)
positive regulation of cell population proliferationEpidermal growth factor receptorHomo sapiens (human)
MAPK cascadeEpidermal growth factor receptorHomo sapiens (human)
ossificationEpidermal growth factor receptorHomo sapiens (human)
embryonic placenta developmentEpidermal growth factor receptorHomo sapiens (human)
positive regulation of protein phosphorylationEpidermal growth factor receptorHomo sapiens (human)
hair follicle developmentEpidermal growth factor receptorHomo sapiens (human)
translationEpidermal growth factor receptorHomo sapiens (human)
signal transductionEpidermal growth factor receptorHomo sapiens (human)
epidermal growth factor receptor signaling pathwayEpidermal growth factor receptorHomo sapiens (human)
activation of phospholipase C activityEpidermal growth factor receptorHomo sapiens (human)
salivary gland morphogenesisEpidermal growth factor receptorHomo sapiens (human)
midgut developmentEpidermal growth factor receptorHomo sapiens (human)
learning or memoryEpidermal growth factor receptorHomo sapiens (human)
circadian rhythmEpidermal growth factor receptorHomo sapiens (human)
positive regulation of cell population proliferationEpidermal growth factor receptorHomo sapiens (human)
diterpenoid metabolic processEpidermal growth factor receptorHomo sapiens (human)
peptidyl-tyrosine phosphorylationEpidermal growth factor receptorHomo sapiens (human)
cerebral cortex cell migrationEpidermal growth factor receptorHomo sapiens (human)
positive regulation of cell growthEpidermal growth factor receptorHomo sapiens (human)
lung developmentEpidermal growth factor receptorHomo sapiens (human)
positive regulation of cell migrationEpidermal growth factor receptorHomo sapiens (human)
positive regulation of superoxide anion generationEpidermal growth factor receptorHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylationEpidermal growth factor receptorHomo sapiens (human)
response to cobalaminEpidermal growth factor receptorHomo sapiens (human)
response to hydroxyisoflavoneEpidermal growth factor receptorHomo sapiens (human)
cellular response to reactive oxygen speciesEpidermal growth factor receptorHomo sapiens (human)
peptidyl-tyrosine autophosphorylationEpidermal growth factor receptorHomo sapiens (human)
ERBB2-EGFR signaling pathwayEpidermal growth factor receptorHomo sapiens (human)
negative regulation of epidermal growth factor receptor signaling pathwayEpidermal growth factor receptorHomo sapiens (human)
negative regulation of protein catabolic processEpidermal growth factor receptorHomo sapiens (human)
vasodilationEpidermal growth factor receptorHomo sapiens (human)
positive regulation of phosphorylationEpidermal growth factor receptorHomo sapiens (human)
ovulation cycleEpidermal growth factor receptorHomo sapiens (human)
hydrogen peroxide metabolic processEpidermal growth factor receptorHomo sapiens (human)
negative regulation of apoptotic processEpidermal growth factor receptorHomo sapiens (human)
positive regulation of MAP kinase activityEpidermal growth factor receptorHomo sapiens (human)
tongue developmentEpidermal growth factor receptorHomo sapiens (human)
positive regulation of cyclin-dependent protein serine/threonine kinase activityEpidermal growth factor receptorHomo sapiens (human)
positive regulation of DNA repairEpidermal growth factor receptorHomo sapiens (human)
positive regulation of DNA replicationEpidermal growth factor receptorHomo sapiens (human)
positive regulation of bone resorptionEpidermal growth factor receptorHomo sapiens (human)
positive regulation of DNA-templated transcriptionEpidermal growth factor receptorHomo sapiens (human)
positive regulation of vasoconstrictionEpidermal growth factor receptorHomo sapiens (human)
negative regulation of mitotic cell cycleEpidermal growth factor receptorHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIEpidermal growth factor receptorHomo sapiens (human)
regulation of JNK cascadeEpidermal growth factor receptorHomo sapiens (human)
symbiont entry into host cellEpidermal growth factor receptorHomo sapiens (human)
protein autophosphorylationEpidermal growth factor receptorHomo sapiens (human)
astrocyte activationEpidermal growth factor receptorHomo sapiens (human)
positive regulation of fibroblast proliferationEpidermal growth factor receptorHomo sapiens (human)
digestive tract morphogenesisEpidermal growth factor receptorHomo sapiens (human)
positive regulation of smooth muscle cell proliferationEpidermal growth factor receptorHomo sapiens (human)
neuron projection morphogenesisEpidermal growth factor receptorHomo sapiens (human)
epithelial cell proliferationEpidermal growth factor receptorHomo sapiens (human)
positive regulation of epithelial cell proliferationEpidermal growth factor receptorHomo sapiens (human)
regulation of peptidyl-tyrosine phosphorylationEpidermal growth factor receptorHomo sapiens (human)
protein insertion into membraneEpidermal growth factor receptorHomo sapiens (human)
response to calcium ionEpidermal growth factor receptorHomo sapiens (human)
regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionEpidermal growth factor receptorHomo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionEpidermal growth factor receptorHomo sapiens (human)
positive regulation of synaptic transmission, glutamatergicEpidermal growth factor receptorHomo sapiens (human)
positive regulation of glial cell proliferationEpidermal growth factor receptorHomo sapiens (human)
morphogenesis of an epithelial foldEpidermal growth factor receptorHomo sapiens (human)
eyelid development in camera-type eyeEpidermal growth factor receptorHomo sapiens (human)
response to UV-AEpidermal growth factor receptorHomo sapiens (human)
positive regulation of mucus secretionEpidermal growth factor receptorHomo sapiens (human)
regulation of ERK1 and ERK2 cascadeEpidermal growth factor receptorHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeEpidermal growth factor receptorHomo sapiens (human)
cellular response to amino acid stimulusEpidermal growth factor receptorHomo sapiens (human)
cellular response to mechanical stimulusEpidermal growth factor receptorHomo sapiens (human)
cellular response to cadmium ionEpidermal growth factor receptorHomo sapiens (human)
cellular response to epidermal growth factor stimulusEpidermal growth factor receptorHomo sapiens (human)
cellular response to estradiol stimulusEpidermal growth factor receptorHomo sapiens (human)
cellular response to xenobiotic stimulusEpidermal growth factor receptorHomo sapiens (human)
cellular response to dexamethasone stimulusEpidermal growth factor receptorHomo sapiens (human)
positive regulation of canonical Wnt signaling pathwayEpidermal growth factor receptorHomo sapiens (human)
liver regenerationEpidermal growth factor receptorHomo sapiens (human)
cell-cell adhesionEpidermal growth factor receptorHomo sapiens (human)
positive regulation of protein kinase C activityEpidermal growth factor receptorHomo sapiens (human)
positive regulation of G1/S transition of mitotic cell cycleEpidermal growth factor receptorHomo sapiens (human)
positive regulation of non-canonical NF-kappaB signal transductionEpidermal growth factor receptorHomo sapiens (human)
positive regulation of prolactin secretionEpidermal growth factor receptorHomo sapiens (human)
positive regulation of miRNA transcriptionEpidermal growth factor receptorHomo sapiens (human)
positive regulation of protein localization to plasma membraneEpidermal growth factor receptorHomo sapiens (human)
negative regulation of cardiocyte differentiationEpidermal growth factor receptorHomo sapiens (human)
neurogenesisEpidermal growth factor receptorHomo sapiens (human)
multicellular organism developmentEpidermal growth factor receptorHomo sapiens (human)
positive regulation of kinase activityEpidermal growth factor receptorHomo sapiens (human)
cell surface receptor protein tyrosine kinase signaling pathwayEpidermal growth factor receptorHomo sapiens (human)
response to singlet oxygenTyrosine-protein kinase FynHomo sapiens (human)
neuron migrationTyrosine-protein kinase FynHomo sapiens (human)
stimulatory C-type lectin receptor signaling pathwayTyrosine-protein kinase FynHomo sapiens (human)
adaptive immune responseTyrosine-protein kinase FynHomo sapiens (human)
negative regulation of inflammatory response to antigenic stimulusTyrosine-protein kinase FynHomo sapiens (human)
heart processTyrosine-protein kinase FynHomo sapiens (human)
protein phosphorylationTyrosine-protein kinase FynHomo sapiens (human)
calcium ion transportTyrosine-protein kinase FynHomo sapiens (human)
G protein-coupled glutamate receptor signaling pathwayTyrosine-protein kinase FynHomo sapiens (human)
axon guidanceTyrosine-protein kinase FynHomo sapiens (human)
learningTyrosine-protein kinase FynHomo sapiens (human)
feeding behaviorTyrosine-protein kinase FynHomo sapiens (human)
regulation of cell shapeTyrosine-protein kinase FynHomo sapiens (human)
gene expressionTyrosine-protein kinase FynHomo sapiens (human)
negative regulation of gene expressionTyrosine-protein kinase FynHomo sapiens (human)
negative regulation of hydrogen peroxide biosynthetic processTyrosine-protein kinase FynHomo sapiens (human)
positive regulation of neuron projection developmentTyrosine-protein kinase FynHomo sapiens (human)
protein ubiquitinationTyrosine-protein kinase FynHomo sapiens (human)
peptidyl-tyrosine phosphorylationTyrosine-protein kinase FynHomo sapiens (human)
protein catabolic processTyrosine-protein kinase FynHomo sapiens (human)
forebrain developmentTyrosine-protein kinase FynHomo sapiens (human)
T cell costimulationTyrosine-protein kinase FynHomo sapiens (human)
negative regulation of protein ubiquitinationTyrosine-protein kinase FynHomo sapiens (human)
intracellular signal transductionTyrosine-protein kinase FynHomo sapiens (human)
cellular response to platelet-derived growth factor stimulusTyrosine-protein kinase FynHomo sapiens (human)
Fc-gamma receptor signaling pathway involved in phagocytosisTyrosine-protein kinase FynHomo sapiens (human)
negative regulation of protein catabolic processTyrosine-protein kinase FynHomo sapiens (human)
positive regulation of tyrosine phosphorylation of STAT proteinTyrosine-protein kinase FynHomo sapiens (human)
response to ethanolTyrosine-protein kinase FynHomo sapiens (human)
vascular endothelial growth factor receptor signaling pathwayTyrosine-protein kinase FynHomo sapiens (human)
ephrin receptor signaling pathwayTyrosine-protein kinase FynHomo sapiens (human)
dendrite morphogenesisTyrosine-protein kinase FynHomo sapiens (human)
regulation of peptidyl-tyrosine phosphorylationTyrosine-protein kinase FynHomo sapiens (human)
activated T cell proliferationTyrosine-protein kinase FynHomo sapiens (human)
modulation of chemical synaptic transmissionTyrosine-protein kinase FynHomo sapiens (human)
T cell receptor signaling pathwayTyrosine-protein kinase FynHomo sapiens (human)
leukocyte migrationTyrosine-protein kinase FynHomo sapiens (human)
detection of mechanical stimulus involved in sensory perception of painTyrosine-protein kinase FynHomo sapiens (human)
cellular response to hydrogen peroxideTyrosine-protein kinase FynHomo sapiens (human)
cellular response to transforming growth factor beta stimulusTyrosine-protein kinase FynHomo sapiens (human)
positive regulation of protein targeting to membraneTyrosine-protein kinase FynHomo sapiens (human)
dendritic spine maintenanceTyrosine-protein kinase FynHomo sapiens (human)
positive regulation of protein localization to nucleusTyrosine-protein kinase FynHomo sapiens (human)
regulation of glutamate receptor signaling pathwayTyrosine-protein kinase FynHomo sapiens (human)
negative regulation of oxidative stress-induced intrinsic apoptotic signaling pathwayTyrosine-protein kinase FynHomo sapiens (human)
negative regulation of dendritic spine maintenanceTyrosine-protein kinase FynHomo sapiens (human)
response to amyloid-betaTyrosine-protein kinase FynHomo sapiens (human)
cellular response to amyloid-betaTyrosine-protein kinase FynHomo sapiens (human)
cellular response to L-glutamateTyrosine-protein kinase FynHomo sapiens (human)
cellular response to glycineTyrosine-protein kinase FynHomo sapiens (human)
positive regulation of protein localization to membraneTyrosine-protein kinase FynHomo sapiens (human)
regulation of calcium ion import across plasma membraneTyrosine-protein kinase FynHomo sapiens (human)
positive regulation of cysteine-type endopeptidase activityTyrosine-protein kinase FynHomo sapiens (human)
innate immune responseTyrosine-protein kinase FynHomo sapiens (human)
cell differentiationTyrosine-protein kinase FynHomo sapiens (human)
cell surface receptor protein tyrosine kinase signaling pathwayTyrosine-protein kinase FynHomo sapiens (human)
cysteine metabolic processCystathionine gamma-lyaseHomo sapiens (human)
lipid metabolic processCystathionine gamma-lyaseHomo sapiens (human)
protein-pyridoxal-5-phosphate linkage via peptidyl-N6-pyridoxal phosphate-L-lysineCystathionine gamma-lyaseHomo sapiens (human)
cysteine biosynthetic process via cystathionineCystathionine gamma-lyaseHomo sapiens (human)
cysteine biosynthetic processCystathionine gamma-lyaseHomo sapiens (human)
transsulfurationCystathionine gamma-lyaseHomo sapiens (human)
endoplasmic reticulum unfolded protein responseCystathionine gamma-lyaseHomo sapiens (human)
positive regulation of canonical NF-kappaB signal transductionCystathionine gamma-lyaseHomo sapiens (human)
protein sulfhydrationCystathionine gamma-lyaseHomo sapiens (human)
protein homotetramerizationCystathionine gamma-lyaseHomo sapiens (human)
hydrogen sulfide biosynthetic processCystathionine gamma-lyaseHomo sapiens (human)
positive regulation of aortic smooth muscle cell differentiationCystathionine gamma-lyaseHomo sapiens (human)
cellular response to leukemia inhibitory factorCystathionine gamma-lyaseHomo sapiens (human)
negative regulation of apoptotic signaling pathwayCystathionine gamma-lyaseHomo sapiens (human)
monoatomic ion transportSolute carrier family 15 member 1Homo sapiens (human)
protein transportSolute carrier family 15 member 1Homo sapiens (human)
peptide transportSolute carrier family 15 member 1Homo sapiens (human)
dipeptide import across plasma membraneSolute carrier family 15 member 1Homo sapiens (human)
tripeptide import across plasma membraneSolute carrier family 15 member 1Homo sapiens (human)
proton transmembrane transportSolute carrier family 15 member 1Homo sapiens (human)
negative regulation of receptor internalizationAtaxin-2Homo sapiens (human)
regulation of translationAtaxin-2Homo sapiens (human)
RNA metabolic processAtaxin-2Homo sapiens (human)
P-body assemblyAtaxin-2Homo sapiens (human)
stress granule assemblyAtaxin-2Homo sapiens (human)
RNA transportAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (60)

Processvia Protein(s)Taxonomy
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)
guanyl-nucleotide exchange factor activityRap guanine nucleotide exchange factor 3Homo sapiens (human)
protein bindingRap guanine nucleotide exchange factor 3Homo sapiens (human)
protein domain specific bindingRap guanine nucleotide exchange factor 3Homo sapiens (human)
cAMP bindingRap guanine nucleotide exchange factor 3Homo sapiens (human)
epidermal growth factor receptor activityEpidermal growth factor receptorHomo sapiens (human)
virus receptor activityEpidermal growth factor receptorHomo sapiens (human)
chromatin bindingEpidermal growth factor receptorHomo sapiens (human)
double-stranded DNA bindingEpidermal growth factor receptorHomo sapiens (human)
MAP kinase kinase kinase activityEpidermal growth factor receptorHomo sapiens (human)
protein tyrosine kinase activityEpidermal growth factor receptorHomo sapiens (human)
transmembrane receptor protein tyrosine kinase activityEpidermal growth factor receptorHomo sapiens (human)
transmembrane signaling receptor activityEpidermal growth factor receptorHomo sapiens (human)
epidermal growth factor receptor activityEpidermal growth factor receptorHomo sapiens (human)
integrin bindingEpidermal growth factor receptorHomo sapiens (human)
protein bindingEpidermal growth factor receptorHomo sapiens (human)
calmodulin bindingEpidermal growth factor receptorHomo sapiens (human)
ATP bindingEpidermal growth factor receptorHomo sapiens (human)
enzyme bindingEpidermal growth factor receptorHomo sapiens (human)
kinase bindingEpidermal growth factor receptorHomo sapiens (human)
protein kinase bindingEpidermal growth factor receptorHomo sapiens (human)
protein phosphatase bindingEpidermal growth factor receptorHomo sapiens (human)
protein tyrosine kinase activator activityEpidermal growth factor receptorHomo sapiens (human)
transmembrane receptor protein tyrosine kinase activator activityEpidermal growth factor receptorHomo sapiens (human)
ubiquitin protein ligase bindingEpidermal growth factor receptorHomo sapiens (human)
identical protein bindingEpidermal growth factor receptorHomo sapiens (human)
cadherin bindingEpidermal growth factor receptorHomo sapiens (human)
actin filament bindingEpidermal growth factor receptorHomo sapiens (human)
ATPase bindingEpidermal growth factor receptorHomo sapiens (human)
epidermal growth factor bindingEpidermal growth factor receptorHomo sapiens (human)
protein tyrosine kinase activityTyrosine-protein kinase FynHomo sapiens (human)
non-membrane spanning protein tyrosine kinase activityTyrosine-protein kinase FynHomo sapiens (human)
protein bindingTyrosine-protein kinase FynHomo sapiens (human)
ATP bindingTyrosine-protein kinase FynHomo sapiens (human)
phospholipase activator activityTyrosine-protein kinase FynHomo sapiens (human)
enzyme bindingTyrosine-protein kinase FynHomo sapiens (human)
type 5 metabotropic glutamate receptor bindingTyrosine-protein kinase FynHomo sapiens (human)
identical protein bindingTyrosine-protein kinase FynHomo sapiens (human)
alpha-tubulin bindingTyrosine-protein kinase FynHomo sapiens (human)
phospholipase bindingTyrosine-protein kinase FynHomo sapiens (human)
transmembrane transporter bindingTyrosine-protein kinase FynHomo sapiens (human)
metal ion bindingTyrosine-protein kinase FynHomo sapiens (human)
ephrin receptor bindingTyrosine-protein kinase FynHomo sapiens (human)
tau protein bindingTyrosine-protein kinase FynHomo sapiens (human)
tau-protein kinase activityTyrosine-protein kinase FynHomo sapiens (human)
growth factor receptor bindingTyrosine-protein kinase FynHomo sapiens (human)
scaffold protein bindingTyrosine-protein kinase FynHomo sapiens (human)
disordered domain specific bindingTyrosine-protein kinase FynHomo sapiens (human)
signaling receptor bindingTyrosine-protein kinase FynHomo sapiens (human)
cystathionine gamma-lyase activityCystathionine gamma-lyaseHomo sapiens (human)
protein bindingCystathionine gamma-lyaseHomo sapiens (human)
calmodulin bindingCystathionine gamma-lyaseHomo sapiens (human)
pyridoxal phosphate bindingCystathionine gamma-lyaseHomo sapiens (human)
identical protein bindingCystathionine gamma-lyaseHomo sapiens (human)
L-cystine L-cysteine-lyase (deaminating)Cystathionine gamma-lyaseHomo sapiens (human)
homocysteine desulfhydrase activityCystathionine gamma-lyaseHomo sapiens (human)
L-cysteine desulfhydrase activityCystathionine gamma-lyaseHomo sapiens (human)
selenocystathionine gamma-lyase activityCystathionine gamma-lyaseHomo sapiens (human)
proton-dependent oligopeptide secondary active transmembrane transporter activitySolute carrier family 15 member 1Homo sapiens (human)
peptide:proton symporter activitySolute carrier family 15 member 1Homo sapiens (human)
tripeptide transmembrane transporter activitySolute carrier family 15 member 1Homo sapiens (human)
dipeptide transmembrane transporter activitySolute carrier family 15 member 1Homo sapiens (human)
RNA bindingAtaxin-2Homo sapiens (human)
epidermal growth factor receptor bindingAtaxin-2Homo sapiens (human)
protein bindingAtaxin-2Homo sapiens (human)
mRNA bindingAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (51)

Processvia Protein(s)Taxonomy
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)
plasma membraneRap guanine nucleotide exchange factor 3Homo sapiens (human)
cortical actin cytoskeletonRap guanine nucleotide exchange factor 3Homo sapiens (human)
plasma membraneRap guanine nucleotide exchange factor 3Homo sapiens (human)
microvillusRap guanine nucleotide exchange factor 3Homo sapiens (human)
endomembrane systemRap guanine nucleotide exchange factor 3Homo sapiens (human)
membraneRap guanine nucleotide exchange factor 3Homo sapiens (human)
lamellipodiumRap guanine nucleotide exchange factor 3Homo sapiens (human)
filopodiumRap guanine nucleotide exchange factor 3Homo sapiens (human)
extracellular exosomeRap guanine nucleotide exchange factor 3Homo sapiens (human)
endosomeEpidermal growth factor receptorHomo sapiens (human)
plasma membraneEpidermal growth factor receptorHomo sapiens (human)
ruffle membraneEpidermal growth factor receptorHomo sapiens (human)
Golgi membraneEpidermal growth factor receptorHomo sapiens (human)
extracellular spaceEpidermal growth factor receptorHomo sapiens (human)
nucleusEpidermal growth factor receptorHomo sapiens (human)
cytoplasmEpidermal growth factor receptorHomo sapiens (human)
endosomeEpidermal growth factor receptorHomo sapiens (human)
endoplasmic reticulum membraneEpidermal growth factor receptorHomo sapiens (human)
plasma membraneEpidermal growth factor receptorHomo sapiens (human)
focal adhesionEpidermal growth factor receptorHomo sapiens (human)
cell surfaceEpidermal growth factor receptorHomo sapiens (human)
endosome membraneEpidermal growth factor receptorHomo sapiens (human)
membraneEpidermal growth factor receptorHomo sapiens (human)
basolateral plasma membraneEpidermal growth factor receptorHomo sapiens (human)
apical plasma membraneEpidermal growth factor receptorHomo sapiens (human)
cell junctionEpidermal growth factor receptorHomo sapiens (human)
clathrin-coated endocytic vesicle membraneEpidermal growth factor receptorHomo sapiens (human)
early endosome membraneEpidermal growth factor receptorHomo sapiens (human)
nuclear membraneEpidermal growth factor receptorHomo sapiens (human)
membrane raftEpidermal growth factor receptorHomo sapiens (human)
perinuclear region of cytoplasmEpidermal growth factor receptorHomo sapiens (human)
multivesicular body, internal vesicle lumenEpidermal growth factor receptorHomo sapiens (human)
intracellular vesicleEpidermal growth factor receptorHomo sapiens (human)
protein-containing complexEpidermal growth factor receptorHomo sapiens (human)
receptor complexEpidermal growth factor receptorHomo sapiens (human)
Shc-EGFR complexEpidermal growth factor receptorHomo sapiens (human)
basal plasma membraneEpidermal growth factor receptorHomo sapiens (human)
membrane raftTyrosine-protein kinase FynHomo sapiens (human)
dendriteTyrosine-protein kinase FynHomo sapiens (human)
nucleusTyrosine-protein kinase FynHomo sapiens (human)
mitochondrionTyrosine-protein kinase FynHomo sapiens (human)
endosomeTyrosine-protein kinase FynHomo sapiens (human)
cytosolTyrosine-protein kinase FynHomo sapiens (human)
actin filamentTyrosine-protein kinase FynHomo sapiens (human)
plasma membraneTyrosine-protein kinase FynHomo sapiens (human)
postsynaptic densityTyrosine-protein kinase FynHomo sapiens (human)
dendriteTyrosine-protein kinase FynHomo sapiens (human)
perikaryonTyrosine-protein kinase FynHomo sapiens (human)
cell bodyTyrosine-protein kinase FynHomo sapiens (human)
membrane raftTyrosine-protein kinase FynHomo sapiens (human)
perinuclear region of cytoplasmTyrosine-protein kinase FynHomo sapiens (human)
perinuclear endoplasmic reticulumTyrosine-protein kinase FynHomo sapiens (human)
glial cell projectionTyrosine-protein kinase FynHomo sapiens (human)
Schaffer collateral - CA1 synapseTyrosine-protein kinase FynHomo sapiens (human)
plasma membraneTyrosine-protein kinase FynHomo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)
cytosolCystathionine gamma-lyaseHomo sapiens (human)
extracellular exosomeCystathionine gamma-lyaseHomo sapiens (human)
cytoplasmCystathionine gamma-lyaseHomo sapiens (human)
plasma membraneSolute carrier family 15 member 1Homo sapiens (human)
brush borderSolute carrier family 15 member 1Homo sapiens (human)
membraneSolute carrier family 15 member 1Homo sapiens (human)
apical plasma membraneSolute carrier family 15 member 1Homo sapiens (human)
plasma membraneSolute carrier family 15 member 1Homo sapiens (human)
apical plasma membraneSolute carrier family 15 member 1Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)
cytoplasmAtaxin-2Homo sapiens (human)
Golgi apparatusAtaxin-2Homo sapiens (human)
trans-Golgi networkAtaxin-2Homo sapiens (human)
cytosolAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
membraneAtaxin-2Homo sapiens (human)
perinuclear region of cytoplasmAtaxin-2Homo sapiens (human)
ribonucleoprotein complexAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (251)

Assay IDTitleYearJournalArticle
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS 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.
AID1079931Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source]
AID1149864Cardiovascular activity in deoxycorticosterone acetate treated hypertensive CD rat assessed as change in heart rate at 50 mg, ip after 4 hrs relative to control1977Journal of medicinal chemistry, Nov, Volume: 20, Issue:11
Synthesis and hypotensive activity of some cyclopentano-1,2,3,4-tetrahydroisoquinolines.
AID588209Literature-mined public compounds from Greene et al multi-species hepatotoxicity modelling dataset2010Chemical research in toxicology, Jul-19, Volume: 23, Issue:7
Developing structure-activity relationships for the prediction of hepatotoxicity.
AID625291Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625279Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID496818Antimicrobial activity against Trypanosoma brucei brucei2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
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.
AID1209457Unbound Cmax in human plasma2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
In vitro inhibition of the bile salt export pump correlates with risk of cholestatic drug-induced liver injury in humans.
AID171152Antihypertensive activity in spontaneously hypertensive rats was measured as average blood pressure at 100 mg/kg, p.o. before predose1980Journal of medicinal chemistry, Dec, Volume: 23, Issue:12
Lipophilic and hydrophilic esters of 4-acetyl-2-(2-hydroxyethyl)-5,6-bis(4-chlorophenyl)-2H-pyridazin-3-one as antihypertensive agents.
AID588214FDA HLAED, liver enzyme composite activity2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1149836Hypotensive activity in deoxycorticosterone acetate treated hypertensive CD rat assessed as change in blood pressure at 50 mg, ip after 4 hrs relative to control1977Journal of medicinal chemistry, Nov, Volume: 20, Issue:11
Synthesis and hypotensive activity of some cyclopentano-1,2,3,4-tetrahydroisoquinolines.
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.
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.
AID625285Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625283Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625289Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID588217FDA HLAED, serum glutamic pyruvic transaminase (SGPT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID171150Antihypertensive activity in spontaneously hypertensive rats was measured as average blood pressure at 100 mg/kg, p.o. after 4 hours of postdose-21980Journal of medicinal chemistry, Dec, Volume: 23, Issue:12
Lipophilic and hydrophilic esters of 4-acetyl-2-(2-hydroxyethyl)-5,6-bis(4-chlorophenyl)-2H-pyridazin-3-one as antihypertensive agents.
AID977602Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID521220Inhibition of neurosphere proliferation of mouse neural precursor cells by MTT assay2007Nature chemical biology, May, Volume: 3, Issue:5
Chemical genetics reveals a complex functional ground state of neural stem cells.
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.
AID625276FDA Liver Toxicity Knowledge Base Benchmark Dataset (LTKB-BD) drugs of most concern for DILI2011Drug discovery today, Aug, Volume: 16, Issue:15-16
FDA-approved drug labeling for the study of drug-induced liver injury.
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.
AID496828Antimicrobial activity against Leishmania donovani2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID185814Antihypertensive activity was evaluated in SH rats by measuring initial mean arterial pressure at 0.24 mM/kg dose administered perorally; equivalent to 50 mg/kg of methyldopa1984Journal of medicinal chemistry, Jun, Volume: 27, Issue:6
3-Hydroxy-alpha-methyltyrosine progenitors: synthesis and evaluation of some (2-oxo-1,3-dioxol-4-yl)methyl esters.
AID1144297Hypotensive effect in conscious spontaneously hypertensive rat assessed as reduction in blood pressure at 100 mg/kg, po administered as single dose1976Journal of medicinal chemistry, Jan, Volume: 19, Issue:1
Amino acids. 1. alpha-Hydroxymethylphenylalanines.
AID409954Inhibition of mouse brain MAOA2008Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
Quantitative structure-activity relationship and complex network approach to monoamine oxidase A and B inhibitors.
AID171142Antihypertensive activity in spontaneously hypertensive rats was measured as average blood pressure at 100 mg/kg, po after 24 hours of postdose-21980Journal of medicinal chemistry, Dec, Volume: 23, Issue:12
Antihypertensive 5,6-diarylpyridazin-3-ones.
AID1149835Hypotensive activity in deoxycorticosterone acetate treated hypertensive CD rat assessed as change in blood pressure at 50 mg, ip after 2 hrs relative to control1977Journal of medicinal chemistry, Nov, Volume: 20, Issue:11
Synthesis and hypotensive activity of some cyclopentano-1,2,3,4-tetrahydroisoquinolines.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID1149834Hypotensive activity in deoxycorticosterone acetate treated hypertensive CD rat assessed as change in blood pressure at 50 mg, ip after 1 hr relative to control1977Journal of medicinal chemistry, Nov, Volume: 20, Issue:11
Synthesis and hypotensive activity of some cyclopentano-1,2,3,4-tetrahydroisoquinolines.
AID588219FDA HLAED, gamma-glutamyl transferase (GGT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID588216FDA HLAED, serum glutamic oxaloacetic transaminase (SGOT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
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?
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID26576pKa 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.
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.
AID625288Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
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.
AID588215FDA HLAED, alkaline phosphatase increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
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.
AID15284Compound was evaluated for its urinary recovery after oral administration (100 mg) to Beagle dogs1984Journal of medicinal chemistry, Jun, Volume: 27, Issue:6
3-Hydroxy-alpha-methyltyrosine progenitors: synthesis and evaluation of some (2-oxo-1,3-dioxol-4-yl)methyl esters.
AID496832Antimicrobial activity against Trypanosoma brucei rhodesiense2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID678714Inhibition of human CYP2C19 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 3-butyryl-7-methoxycoumarin as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID1144296Hypotensive effect in conscious spontaneously hypertensive rat assessed as reduction in blood pressure at 50 mg/kg, po administered as single dose1976Journal of medicinal chemistry, Jan, Volume: 19, Issue:1
Amino acids. 1. alpha-Hydroxymethylphenylalanines.
AID496819Antimicrobial activity against Plasmodium falciparum2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID496830Antimicrobial activity against Leishmania major2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
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.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID1149837Hypotensive activity in deoxycorticosterone acetate treated hypertensive CD rat assessed as change in blood pressure at 50 mg, ip after 24 hrs relative to control1977Journal of medicinal chemistry, Nov, Volume: 20, Issue:11
Synthesis and hypotensive activity of some cyclopentano-1,2,3,4-tetrahydroisoquinolines.
AID1079936Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source]
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.
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.
AID157601ability to inhibit the decarboxylation of L-phenyl-alanine using a crude enzyme preparation of phenylalanine decarboxylase (PAD) from Streptococcus faecalis, at 1.76 mM concentration1980Journal of medicinal chemistry, Jul, Volume: 23, Issue:7
Conformationally defined aromatic amino acids. Synthesis and stereochemistry of 2-endo- and 2-exo-amino-1,2,3,4-tetrahydro-1,4-ethanonaphthalene-2-carboxylic acids (2-endo- and 2-exo-aminobenzobicycle[2.2.2]octene-2-carboxylic acids).
AID1079945Animal toxicity known. [column 'TOXIC' in source]
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.
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.
AID592681Apparent permeability across human Caco2 cell membrane after 2 hrs by LC-MS/MS analysis2011Bioorganic & medicinal chemistry, Apr-15, Volume: 19, Issue:8
QSAR-based permeability model for drug-like compounds.
AID681113TP_TRANSPORTER: inhibition of L-tryptophan uptake in Xenopus laevis oocytes2001The Journal of biological chemistry, May-18, Volume: 276, Issue:20
Expression cloning of a Na+-independent aromatic amino acid transporter with structural similarity to H+/monocarboxylate transporters.
AID588218FDA HLAED, lactate dehydrogenase (LDH) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID977599Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
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.
AID678716Inhibition of human CYP3A4 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using diethoxyfluorescein as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID678717Inhibition of human CYP3A4 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 7-benzyloxyquinoline as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
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.
AID678712Inhibition of human CYP1A2 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using ethoxyresorufin as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID496824Antimicrobial activity against Toxoplasma gondii2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
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?
AID678715Inhibition of human CYP2D6 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 4-methylaminoethyl-7-methoxycoumarin as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID496820Antimicrobial activity against Trypanosoma brucei2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID497005Antimicrobial activity against Pneumocystis carinii2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID20499Compound was evaluated for its renal clearance after oral administration (100 mg) to Beagle dogs1984Journal of medicinal chemistry, Jun, Volume: 27, Issue:6
3-Hydroxy-alpha-methyltyrosine progenitors: synthesis and evaluation of some (2-oxo-1,3-dioxol-4-yl)methyl esters.
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.
AID11139Compound was evaluated for its bioavailability after oral administration (100 mg) to Beagle dogs1984Journal of medicinal chemistry, Jun, Volume: 27, Issue:6
3-Hydroxy-alpha-methyltyrosine progenitors: synthesis and evaluation of some (2-oxo-1,3-dioxol-4-yl)methyl esters.
AID678713Inhibition of human CYP2C9 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 7-methoxy-4-trifluoromethylcoumarin-3-acetic acid as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID625281Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID171139Antihypertensive activity in spontaneously hypertensive rats was measured as average blood pressure at 100 mg/kg, p.o. after 24 hours of postdose-1.1980Journal of medicinal chemistry, Dec, Volume: 23, Issue:12
Antihypertensive 5,6-diarylpyridazin-3-ones.
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.
AID588210Human drug-induced liver injury (DILI) modelling dataset from Ekins et al2010Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 38, Issue:12
A predictive ligand-based Bayesian model for human drug-induced liver injury.
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.
AID409956Inhibition of mouse brain MAOB2008Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
Quantitative structure-activity relationship and complex network approach to monoamine oxidase A and B inhibitors.
AID625280Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID179758In vitro inhibition of LTB4 (LT)production in rat blood; ND=No data1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Indazolinones, a new series of redox-active 5-lipoxygenase inhibitors with built-in selectivity and oral activity.
AID15626Systemic availability with respect to methyldopa was determined1984Journal of medicinal chemistry, Jun, Volume: 27, Issue:6
3-Hydroxy-alpha-methyltyrosine progenitors: synthesis and evaluation of some (2-oxo-1,3-dioxol-4-yl)methyl esters.
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.
AID496825Antimicrobial activity against Leishmania mexicana2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID496823Antimicrobial activity against Trichomonas vaginalis2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID19546Terminal elimination from the half life calculated1984Journal of medicinal chemistry, Jun, Volume: 27, Issue:6
3-Hydroxy-alpha-methyltyrosine progenitors: synthesis and evaluation of some (2-oxo-1,3-dioxol-4-yl)methyl esters.
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID171151Antihypertensive activity in spontaneously hypertensive rats was measured as average blood pressure at 100 mg/kg, p.o. before predose1980Journal of medicinal chemistry, Dec, Volume: 23, Issue:12
Antihypertensive 5,6-diarylpyridazin-3-ones.
AID496829Antimicrobial activity against Leishmania infantum2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID625290Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID171145Antihypertensive activity in spontaneously hypertensive rats was measured as average blood pressure at 100 mg/kg, p.o. after 4 hours of postdose-11980Journal of medicinal chemistry, Dec, Volume: 23, Issue:12
Antihypertensive 5,6-diarylpyridazin-3-ones.
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?
AID496817Antimicrobial activity against Trypanosoma cruzi2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
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?
AID171140Antihypertensive activity in spontaneously hypertensive rats was measured as average blood pressure at 100 mg/kg, p.o. after 24 hours of postdose-11980Journal of medicinal chemistry, Dec, Volume: 23, Issue:12
Lipophilic and hydrophilic esters of 4-acetyl-2-(2-hydroxyethyl)-5,6-bis(4-chlorophenyl)-2H-pyridazin-3-one as antihypertensive agents.
AID781325pKa (acid-base dissociation constant) as determined by Liao ref: J Chem Info Model 20092014Pharmaceutical research, Apr, Volume: 31, Issue:4
Comparison of the accuracy of experimental and predicted pKa values of basic and acidic compounds.
AID588208Literature-mined public compounds from Lowe et al phospholipidosis modelling dataset2010Molecular pharmaceutics, Oct-04, Volume: 7, Issue:5
Predicting phospholipidosis using machine learning.
AID116921Compound was tested for toxicity (lethal dose) in male white swiss mice1980Journal of medicinal chemistry, Dec, Volume: 23, Issue:12
Synthetic and preliminary hemodynamic and whole animal toxicity studies on (R,S)-, (R)-, and (S)-2-methyl-3-(2,4,5-trihydroxyphenyl)alanine.
AID1079938Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
AID1149865Cardiovascular activity in deoxycorticosterone acetate treated hypertensive CD rat assessed as change in heart rate at 50 mg, ip after 24 hrs relative to control1977Journal of medicinal chemistry, Nov, Volume: 20, Issue:11
Synthesis and hypotensive activity of some cyclopentano-1,2,3,4-tetrahydroisoquinolines.
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.
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.
AID171149Antihypertensive activity in spontaneously hypertensive rats was measured as average blood pressure at 100 mg/kg, p.o. after 4 hours of postdose-21980Journal of medicinal chemistry, Dec, Volume: 23, Issue:12
Antihypertensive 5,6-diarylpyridazin-3-ones.
AID588220Literature-mined public compounds from Kruhlak et al phospholipidosis modelling dataset2008Toxicology mechanisms and methods, , Volume: 18, Issue:2-3
Development of a phospholipidosis database and predictive quantitative structure-activity relationship (QSAR) models.
AID171143Antihypertensive activity in spontaneously hypertensive rats was measured as average blood pressure at 100 mg/kg, p.o. after 24 hours of postdose-21980Journal of medicinal chemistry, Dec, Volume: 23, Issue:12
Lipophilic and hydrophilic esters of 4-acetyl-2-(2-hydroxyethyl)-5,6-bis(4-chlorophenyl)-2H-pyridazin-3-one as antihypertensive agents.
AID625292Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1209456Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
In vitro inhibition of the bile salt export pump correlates with risk of cholestatic drug-induced liver injury in humans.
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.
AID496827Antimicrobial activity against Leishmania amazonensis2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
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.
AID386623Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells at 100 uM by confocal microscopy2008Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19
Structural requirements for drug inhibition of the liver specific human organic cation transport protein 1.
AID20500Compound was evaluated for its renal clearance after oral administration (200 mg) to Beagle dogs1984Journal of medicinal chemistry, Jun, Volume: 27, Issue:6
3-Hydroxy-alpha-methyltyrosine progenitors: synthesis and evaluation of some (2-oxo-1,3-dioxol-4-yl)methyl esters.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID625287Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID496831Antimicrobial activity against Cryptosporidium parvum2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID567091Drug absorption in human assessed as human intestinal absorption rate2011European journal of medicinal chemistry, Jan, Volume: 46, Issue:1
Prediction of drug intestinal absorption by new linear and non-linear QSPR.
AID1149863Cardiovascular activity in deoxycorticosterone acetate treated hypertensive CD rat assessed as change in heart rate at 50 mg, ip after 2 hrs relative to control1977Journal of medicinal chemistry, Nov, Volume: 20, Issue:11
Synthesis and hypotensive activity of some cyclopentano-1,2,3,4-tetrahydroisoquinolines.
AID1149862Cardiovascular activity in deoxycorticosterone acetate treated hypertensive CD rat assessed as change in heart rate at 50 mg, ip after 1 hr relative to control1977Journal of medicinal chemistry, Nov, Volume: 20, Issue:11
Synthesis and hypotensive activity of some cyclopentano-1,2,3,4-tetrahydroisoquinolines.
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID425653Renal clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
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?
AID11140Compound was evaluated for its bioavailability after oral administration (200 mg) to Beagle dogs1984Journal of medicinal chemistry, Jun, Volume: 27, Issue:6
3-Hydroxy-alpha-methyltyrosine progenitors: synthesis and evaluation of some (2-oxo-1,3-dioxol-4-yl)methyl esters.
AID496821Antimicrobial activity against Leishmania2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID425652Total body clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID625282Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID171146Antihypertensive activity in spontaneously hypertensive rats was measured as average blood pressure at 100 mg/kg, p.o. after 4 hours of postdose-11980Journal of medicinal chemistry, Dec, Volume: 23, Issue:12
Lipophilic and hydrophilic esters of 4-acetyl-2-(2-hydroxyethyl)-5,6-bis(4-chlorophenyl)-2H-pyridazin-3-one as antihypertensive agents.
AID1209455Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
In vitro inhibition of the bile salt export pump correlates with risk of cholestatic drug-induced liver injury in humans.
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.
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.
AID496826Antimicrobial activity against Entamoeba histolytica2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1079935Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
AID678720Metabolic stability in human liver microsomes assessed as low signal/noise ratio (S/N of 1 to 10) by measuring GSH adduct formation at 100 uM after 90 mins by HPLC-MS analysis2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID625284Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
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.
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.
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.
AID15285Compound was evaluated for its urinary recovery after oral administration (200 mg) to Beagle dogs1984Journal of medicinal chemistry, Jun, Volume: 27, Issue:6
3-Hydroxy-alpha-methyltyrosine progenitors: synthesis and evaluation of some (2-oxo-1,3-dioxol-4-yl)methyl esters.
AID540235Phospholipidosis-negative literature compound
AID681608TP_TRANSPORTER: inhibition of Gly-Sar uptake (Gly-Sar: 20 uM) in PEPT1-expressing CHO cells1999Journal of pharmaceutical sciences, Mar, Volume: 88, Issue:3
CHO/hPEPT1 cells overexpressing the human peptide transporter (hPEPT1) as an alternative in vitro model for peptidomimetic drugs.
AID625286Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1079933Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is
AID19545Terminal elimination from the half life calculated1984Journal of medicinal chemistry, Jun, Volume: 27, Issue:6
3-Hydroxy-alpha-methyltyrosine progenitors: synthesis and evaluation of some (2-oxo-1,3-dioxol-4-yl)methyl esters.
AID678722Covalent binding affinity to human liver microsomes assessed per mg of protein at 10 uM after 60 mins presence of NADPH2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
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?
AID186057Antihypertensive activity was evaluated in SH rats by measuring imax reduction in mean arterial pressure at 0.24 mM/kg dose administered perorally; equivalent to 50 mg/kg of methyldopa1984Journal of medicinal chemistry, Jun, Volume: 27, Issue:6
3-Hydroxy-alpha-methyltyrosine progenitors: synthesis and evaluation of some (2-oxo-1,3-dioxol-4-yl)methyl esters.
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.
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.
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.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
AID588378qHTS for Inhibitors of ATXN expression: Validation
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.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
AID1347050Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347049Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
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.
AID1347045Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
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.
AID504836Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation2002The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16
Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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).
AID1159550Human Phosphogluconate dehydrogenase (6PGD) Inhibitor Screening2015Nature cell biology, Nov, Volume: 17, Issue:11
6-Phosphogluconate dehydrogenase links oxidative PPP, lipogenesis and tumour growth by inhibiting LKB1-AMPK signalling.
AID1800301Human CSE enzyme assay from Article 10.1021/cb500009r: \\Novel inhibitors of human DOPA decarboxylase extracted from Euonymus glabra Roxb.\\2014ACS chemical biology, Apr-18, Volume: 9, Issue:4
Novel inhibitors of human DOPA decarboxylase extracted from Euonymus glabra Roxb.
AID1800300DDC-MDH-PEPC-Linked assay from Article 10.1021/cb500009r: \\Novel inhibitors of human DOPA decarboxylase extracted from Euonymus glabra Roxb.\\2014ACS chemical biology, Apr-18, Volume: 9, Issue:4
Novel inhibitors of human DOPA decarboxylase extracted from Euonymus glabra Roxb.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
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.
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.
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.
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.
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.
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.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
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.
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.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
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.
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (3,450)

TimeframeStudies, This Drug (%)All Drugs %
pre-19902970 (86.09)18.7374
1990's195 (5.65)18.2507
2000's113 (3.28)29.6817
2010's131 (3.80)24.3611
2020's41 (1.19)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 91.18

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

MetricThis Compound (vs All)
Research Demand Index91.18 (24.57)
Research Supply Index2.40 (2.92)
Research Growth Index4.55 (4.65)
Search Engine Demand Index156.88 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (91.18)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials420 (11.29%)5.53%
Trials0 (0.00%)5.53%
Reviews335 (9.01%)6.00%
Reviews0 (0.00%)6.00%
Case Studies298 (8.01%)4.05%
Case Studies0 (0.00%)4.05%
Observational4 (0.11%)0.25%
Observational0 (0.00%)0.25%
Other2,662 (71.58%)84.16%
Other10 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (18)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Effectiveness Of Anti-Hypertensive Treatment In Stable Pregnant Women With Severe Pre-Eclampsia: Randomized Placebo-Controlled Clinical Trial [NCT01361425]Phase 4200 participants (Anticipated)Interventional2011-05-31Recruiting
Personalized Hemodynamically Guided Antihypertensive Treatment in Pregnant Women With Mild to Moderate Hypertension: a Randomized Controlled Trial [NCT02531490]Phase 4368 participants (Anticipated)Interventional2015-01-01Recruiting
Open Label Pilot Study of the Effect of Methyldopa on MHC-II Antigen Presentation in Type 1 Diabetes [NCT01883804]30 participants (Actual)Interventional2013-06-30Completed
Methyldopa for Reduction of DQ8 Antigen Presentation in At-Risk Subjects for Type 1 Diabetes Mellitus [NCT03396484]Phase 20 participants (Actual)Interventional2020-09-30Withdrawn(stopped due to Study not begun due to continued laboratory work on the feasibility of outcome measures.)
Association Between Angiotensin Converting Enzyme Inhibitor or Angiotensin Receptor Blocker Use and COVID-19 Severity and Mortality Among US Veterans [NCT04467931]22,213 participants (Actual)Observational2020-01-19Completed
Effect of Foot Reflexology on Preeclampsia [NCT05888896]60 participants (Anticipated)Interventional2023-06-09Recruiting
The Pathophysiology of Orthostatic Hypotension [NCT00748059]Phase 110 participants (Actual)Interventional1996-12-31Completed
A Phase 1b, Randomized, Single-blind, Placebo-controlled, Multiple Ascending Dose (MAD) Study to Assess the Steady-State Pharmacokinetics and DQ8 Blocking Efficacy of Orally Administered IMT-002 in Patients With Type 1 Diabetes and HLA-DQ8 [NCT04625595]Phase 130 participants (Actual)Interventional2020-11-09Completed
The CLIP (Community Level Interventions for Pre-eclampsia) Cluster Randomized Controlled Trial [NCT01911494]87,500 participants (Anticipated)Interventional2013-09-30Completed
Oral Antihypertensive Regimens for Management of Hypertension in Pregnancy [NCT01912677]Phase 4894 participants (Actual)Interventional2015-04-30Completed
Autonomic Nervous System and Chronic Fatigue Syndrome [NCT00580619]Phase 1170 participants (Actual)Interventional2007-04-30Completed
Management of Hypertension in the Early Postpartum Period: Randomized Clinical Trial Comparing Two Antihypertensive Medications [NCT04835233]Phase 4180 participants (Actual)Interventional2021-05-01Completed
Cardiovascular Performance and Autonomic Reactivity in Formerly Preeclamptic Women With a Contracted Plasma Volume (CAPACITY Trial) [NCT00117546]Phase 435 participants (Anticipated)Interventional2005-09-30Recruiting
Treatment Targets for Chronic Hypertension in Pregnancy [NCT00194974]Phase 1/Phase 20 participants (Actual)Interventional2004-07-31Withdrawn(stopped due to Lack of funding)
Clinical Bioequivalence Study on Two Methyldopa Tablet 250mg Formulations [NCT03210025]Phase 117 participants (Actual)Interventional2017-09-20Completed
A Comparison of Compliance Between Clonidine Patch and Methyldopa for the Treatment of Chronic Hypertension in Pregnancy [NCT00329511]0 participants (Actual)Interventional2004-09-30Withdrawn(stopped due to Feasibility of study. PI termination)
Prevalence of High Plasmatic 3-O-Methyldopa Level in a Specific Population of Patients With a Symptomatology Compatible With AADC Deficiency (Aromatic L-Amino Acid Decarboxylase) [NCT05211609]388 participants (Anticipated)Interventional2022-05-20Recruiting
[NCT01674127]Phase 250 participants (Actual)Interventional2011-08-31Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT01883804 (4) [back to overview]The Change From Baseline of DQ8 Antigen Presentation by Peripheral Blood Mononuclear Cells After 6 Weeks of Methyldopa Treatment.
NCT01883804 (4) [back to overview]The Change in C-Peptide AUC Following a MMTT From Baseline to Study Completion.
NCT01883804 (4) [back to overview]The Change in Hemoglobin A1c From Baseline to Study Completion.
NCT01883804 (4) [back to overview]The Change in Insulin Use From Baseline to Study Completion.

The Change From Baseline of DQ8 Antigen Presentation by Peripheral Blood Mononuclear Cells After 6 Weeks of Methyldopa Treatment.

Cryopreserved primary peripheral blood mononuclear cells were used as antigen presenting cells to stimulate engineered T-cells (T-cell receptor transductant) responding to a specific peptide presented by HLA-DQ8. Secreted IL-2 from the engineered T-cell was measured by a highly sensitive ELISA. This was done for both an α-gliadin/DQ8 responding T-cell and a separate insulin/DQ8 responding T-cell. (NCT01883804)
Timeframe: 6 Weeks (Baseline and week 6)

Interventionpg/mL (Least Squares Mean)
Baseline, α-gliadin/DQ86 weeks of treatment, α-gliadin/DQ8Baseline, insulin/DQ86 weeks of treatment, insulin/DQ8
Study Group64243027.417.9

[back to top]

The Change in C-Peptide AUC Following a MMTT From Baseline to Study Completion.

Investigators aim to observe changes in residual endogenous insulin production as measured by C-peptide 2 hour area under the curve following a Mixed Meal Tolerance Test (MMTT). C-peptide is a measure of endogenous insulin secretion as both are secreted in a 1:1 molar ratio. Individuals ingested a liquid meal (Boost) with a fixed amount of protein, fat and carbohydrate in the fasting state followed by the timed measurements of serum C-peptide at 0, 15, 30, 60, 90 and 120 minutes to compute the AUC. (NCT01883804)
Timeframe: 12 weeks (Baseline and week 12)

Interventionnmol/L/min (Mean)
BaselineStudy Completion
Study Group0.60.7

[back to top]

The Change in Hemoglobin A1c From Baseline to Study Completion.

Investigators aim to observe changes in hemoglobin A1c values, a measure of average blood glucose over the preceding 3 months. (NCT01883804)
Timeframe: 12 weeks (Baseline and week 12)

Interventionpercentage (Mean)
BaselineStudy Completion
Study Group7.46.5

[back to top]

The Change in Insulin Use From Baseline to Study Completion.

Exogenous insulin use per kg of body weight. (NCT01883804)
Timeframe: 12 weeks (Baseline and week 12)

Interventionunits/Kg body weight (Mean)
BaselineStudy Completion
Study Group0.370.36

[back to top]