Page last updated: 2024-11-04

carisoprodol

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

Description

Carisoprodol: A centrally acting skeletal muscle relaxant whose mechanism of action is not completely understood but may be related to its sedative actions. It is used as an adjunct in the symptomatic treatment of musculoskeletal conditions associated with painful muscle spasm. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1202) [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

carisoprodol : A carbamate ester that is the mono-N-isopropyl derivative of meprobamate (which is a significant metabolite). Carisoprodol interrupts neuronal communication within the reticular formation and spinal cord, resulting in sedation and alteration in pain perception. It is used as a muscle relaxant in the symptomatic treatment of musculoskeletal conditions associated with painful muscle spasm. [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 CID2576
CHEMBL ID1233
CHEBI ID3419
SCHEMBL ID33286
MeSH IDM0003488

Synonyms (237)

Synonym
AC-212
carisoprodolum
2-[(carbamoyloxy)methyl]-2-methylpentyl propan-2-ylcarbamate
MLS001148409
AKOS015842914
isopropylcarbamic acid, ester with 2-(hydroxymethyl)-2-methylpentyl carbamate
wln: zvo1x3&1&1ovmy1&1
flexal
soma
carbamic acid, ester with 2-(hydroxymethyl)-2-methylpentylisopropyl carbamate
carlsoma
skutamil
atonalyt
domarax
carbamic acid,3-propanediol isopropylcarbamate
izoprotan
nospasm
apesan
n-isopropyl-2-methyl-2-propyl-1, dicarbamate
isopropyl meprobamate
tonolyt isopropyl meprobamate
cb 8019
mioril
brianil
mioratrina
arusal
miolisodol
diolene
carisoprodate
flexartal
carsodal
somadril
calenfa
somanil
isoprotan
carlsoprol
somalgit
carlsodol
mioriodol
miolisodal
relasom
sanoma
sch 7307
nci-c56235
mediquil
isoprotane
isoprothane
carisol
flexartel
stialgin
carisoma
2-methyl-2-propyl-1,3-propanediol carbamate isopropylcarbamate
carisoprodatum
1, 2-methyl-2-propyl-, carbamate isopropylcarbamate
isomeprobamate
caprodat
nsc-172124
nsc172124
rela
isobamate
carbamic acid, (1-methylethyl)-, 2-[[(aminocarbonyl)oxy]methyl]-2-methylpentyl ester
MLS000028401 ,
smr000058433
DIVK1C_000816
KBIO1_000816
EU-0100319
SPECTRUM_000102
LOPAC0_000319
BSPBIO_000406
PRESTWICK_50
cas-78-44-4
PRESTWICK2_000423
BSPBIO_001935
IDI1_000816
PRESTWICK3_000423
SPECTRUM5_000661
NCGC00089734-02
AB00051932
ccris 4764
caridolin
chinchen
meprodat
flexagilt
einecs 201-118-7
flexagit
fibrosona
neotica
flexidon
(+-)-2-methyl-2-propyl-1,3-propanediol carbamate isopropylcarbamate
1,3-propanediol, 2-methyl-2-propyl-, carbamate isopropylcarbamate (ester)
carsodol
carbamic acid, ester with 2-methyl-2-propyl-1,3-propanediol isopropylcarbamate
brn 1791537
listaflex
carbamic acid, (1-methylethyl)-, 2-(((aminocarbonyl)oxy)methyl)-2-methylpentyl ester
scutamil-c
n-isopropyl-2-methyl-2-propyl-1,3-propanediol dicarbamate
nsc 172124
carisoprodolo [dcit]
carbamic acid, ester with 2-(hydroxymethyl)-2-methylpentyl isopropylcarbamate
artifar
hsdb 3021
carbamic acid, isopropyl-, 2-(hydroxymethyl)-2-methylpentyl ester carbamate (ester)
muslax
carisoprodol
78-44-4
n-isopropy-2-methyl-2-propyl-1,3-propanediol dicarbamate
(1-methylethyl)carbamic acid 2-(((aminocarbonyl)oxy)methyl)-2-methylpentyl ester
isopropylmeprobamate
(rs)-2-{[(aminocarbonyl)oxy]methyl}-2-methylpentyl isopropylcarbamate
(+/-)-2-methyl-2-propyl-1,3-propanediol carbamate isopropylcarbamate
DB00395
2-methyl-2-propyltrimethylene carbamate isopropylcarbamate
carbamic acid 2-isopropylcarbamoyloxymethyl-2-methyl-pentyl ester
carisoprodol (jan/usp/inn)
D00768
soma (tn)
BPBIO1_000448
NCGC00089734-04
NCGC00089734-05
NCGC00089734-07
carisoprodolum [inn-latin]
KBIO3_001155
KBIO2_003110
KBIOSS_000542
KBIO2_005678
KBIO2_000542
KBIOGR_000730
PRESTWICK0_000423
PRESTWICK1_000423
SPBIO_001105
SPECTRUM3_000328
SPBIO_002345
NINDS_000816
SPECTRUM4_000265
SPECTRUM2_001153
SPECTRUM1500162
2-{[(aminocarbonyl)oxy]methyl}-2-methylpentyl isopropylcarbamate
NCGC00089734-06
NCGC00089734-03
NCGC00015278-05
C 8759
HMS2091A06
NCGC00015278-11
CHEMBL1233
chebi:3419 ,
carisoprodol civ
MLS002454391
HMS502I18
FT-0656125
HMS1920K03
HMS1569E08
[2-(carbamoyloxymethyl)-2-methylpentyl] n-propan-2-ylcarbamate
NCGC00015278-09
HMS3259O15
HMS2096E08
tox21_200623
NCGC00258177-01
nsc756671
nsc-756671
pharmakon1600-01500162
tox21_110122
dtxcid904733
dtxsid8024733 ,
HMS2234F13
CCG-40092
NCGC00015278-06
NCGC00015278-04
NCGC00015278-12
NCGC00015278-03
NCGC00015278-07
NCGC00015278-08
21925k482h ,
prazolamine
dea no. 8192
carisoprodolo
unii-21925k482h
carisoprodol [usp:inn:ban]
FT-0601536
NCGC00015278-14
LP00319
HMS3372H19
soma compound component carisoprodol
carisoprodol component of carisoprodol compound
carisoprodol civ [usp-rs]
carisoprodol [hsdb]
carisoprodol compound component carisoprodol
carisoprodol [mi]
carisoprodol [mart.]
carisoprodol [usp monograph]
carisoprodol [orange book]
carisoprodol [ep impurity]
carisoprodol [jan]
carisoprodol [inn]
carisoprodol [who-dd]
carisoprodol [vandf]
carisoprodol component of soma compound
gtpl7610
NC00502
SCHEMBL33286
NCGC00015278-15
tox21_110122_1
carbamic acid, isopropyl-, 2-(hydroxymethyl)-2-methylpentyl ester carbamate
1,3-propanediol, 2-methyl-2-propyl-, carbamate isopropylcarbamate
n-isopropyl-2-methyl-2-propyl-1,3-propanediol, dicarbamate
carbamic acid, isopropyl-, 2-(hydroxymethyl)-2-methylpentyl ester, carbamate
CS-4819
W-104280
HY-B1380
OPERA_ID_1100
AB00051932_15
mfcd00057661
sr-01000000076
SR-01000000076-2
carisoprodol, united states pharmacopeia (usp) reference standard
carisoprodol, european pharmacopoeia (ep) reference standard
carisoprodol 1.0 mg/ml in methanol
SR-01000000076-6
SR-01000000076-4
SBI-0050307.P004
HMS3713E08
2-((carbamoyloxy)methyl)-2-methylpentyl isopropylcarbamate
Q416905
SDCCGSBI-0050307.P005
C3573
carisoprodol civ (usp-rs)
carbamic acid, ester with 2-(hydroxymethyl)-2-methylpentylisoproplylcarbamate
carisoprodol (usp monograph)
carisoprodol (usp:inn:ban)
carisoprodolum (inn-latin)
carisoprodol (mart.)
m03ba02
(rs)-2-(((aminocarbonyl)oxy)methyl)-2-methylpentyl isopropylcarbamate
2-((carbamoyloxy)methyl)-2-methylpentyl propan-2-ylcarbamate
carisoprodol tablets
carisoprodol (ep impurity)
carisoprodol, 1mg/ml in methanol

Research Excerpts

Overview

Carisoprodol (Soma®) is a centrally-acting skeletal-muscle relaxant frequently prescribed for treatment of acute musculoskeletal conditions. The main metabolite, meprobamate, is a controlled substance in the United States due to its sedative properties and potential for abuse.

ExcerptReferenceRelevance
"Carisoprodol (Soma®) is a centrally-acting skeletal-muscle relaxant frequently prescribed for treatment of acute musculoskeletal conditions. "( Carisoprodol pharmacokinetics and distribution in the nucleus accumbens correlates with behavioral effects in rats independent from its metabolism to meprobamate.
Carbonaro, TM; Forster, MJ; Gatch, MB; Nguyen, V; Prokai, L, 2020
)
3.44
"Carisoprodol is a relaxant muscular-skeleton associated with sore muscles and appropriate studies have not been performed on carisoprodol effects on fetuses and mothers. "( Toxicity of Somadril Compound on Fetal Ileum Tissues of Albino Rats.
Ahmed Abd Rabou, M; Alhumaidi Alotaibi, M, 2021
)
2.06
"Carisoprodol is a skeletal muscle relaxant prescribed to treat pain. "( Factors affecting carisoprodol metabolism in pain patients using urinary excretion data.
Atayee, RS; Best, BM; Ma, JD; Tse, SA, 2014
)
2.18
"Carisoprodol is a widely prescribed muscle relaxant, abuse of which has grown considerably in recent years. "( Assessment of subunit-dependent direct gating and allosteric modulatory effects of carisoprodol at GABA(A) receptors.
Dillon, GH; González, LA; Kumar, M, 2015
)
2.08
"Carisoprodol is a widely prescribed muscle relaxant and is also a drug known to be a subject to abuse. "( Pharmacokinetic modeling of carisoprodol and meprobamate disposition in adults.
Lewandowski, TA, 2017
)
2.19
"Carisoprodol is a frequently prescribed muscle relaxant. "( Carisoprodol-mediated modulation of GABAA receptors: in vitro and in vivo studies.
Bell-Horner, CL; Dillon, GH; Forster, MJ; Gatch, MB; Gonzalez, LA; Taylor, CM, 2009
)
3.24
"Carisoprodol is a centrally acting muscle relaxant used in the treatment of various musculoskeletal disorders whose main metabolite, meprobamate, is a controlled substance in the United States due to its sedative properties and potential for abuse."( Carisoprodol withdrawal after internet purchase.
Agrwal, N; Eleid, MF; Goodman, BP; Krahn, LE, 2010
)
3.25
"Carisoprodol withdrawal is an important and under-recognized syndrome that should be considered in patients presenting with neurologic symptoms who are taking the medication. "( Carisoprodol withdrawal after internet purchase.
Agrwal, N; Eleid, MF; Goodman, BP; Krahn, LE, 2010
)
3.25
"Carisoprodol is a centrally acting drug used to relieve skeletal muscle spasms and associated pain in acute musculoskeletal conditions. "( Characterizing the subjective and psychomotor effects of carisoprodol in healthy volunteers.
Coalson, DW; Paice, JA; Zacny, JP, 2011
)
2.06
"Carisoprodol is a muscle relaxant that acts at the GABA(A) receptor. "( Carisoprodol tolerance and precipitated withdrawal.
Carbonaro, T; Forster, MJ; Gatch, MB; Nguyen, JD, 2012
)
3.26
"Carisoprodol is a therapeutic and occasionally abused centrally acting muscle relaxant. "( Postmortem carisoprodol and meprobamate concentrations in blood and liver: lack of significant redistribution.
Lucas, J; McIntyre, IM; Sherrard, J, 2012
)
2.21
"Carisoprodol is a centrally acting skeletal muscle relaxant of which meprobamate, a controlled substance, is the primary active metabolite. "( Carisoprodol: update on abuse potential and legal status.
Burke, RS; Kose, S; Reeves, RR, 2012
)
3.26
"Carisoprodol is a commonly used skeletal muscle relaxant with potential for abuse because of its active metabolite, meprobamate, and several reports have suggested that patients abruptly stopping intake of carisoprodol may have a withdrawal syndrome. "( Somatic dysfunction during carisoprodol cessation: evidence for a carisoprodol withdrawal syndrome.
Parker, JD; Reeves, RR, 2003
)
2.06
"Carisoprodol is a centrally acting muscle relaxant commonly used for lower back pain. "( Impairment due to intake of carisoprodol.
Bramness, JG; Mørland, J; Skurtveit, S, 2004
)
2.06
"Carisoprodol (CSP) is a musculoskeletal relaxant whose active metabolite is meprobamate (MPB). "( Simultaneous determination of carisoprodol and meprobamate in human hair using solid-phase extraction and gas chromatography/mass spectrometry of the trimethylsilyl derivatives.
Chung, BC; In, MK; Kim, JY; Paeng, KJ, 2005
)
2.06
"Carisoprodol is a commonly used centrally acting muscle relaxant. "( Is the frequency of carisoprodol withdrawal syndrome increasing?
Hammer, JS; Pendarvis, RO; Reeves, RR, 2007
)
2.11
"Carisoprodol is a muscle relaxant indicated as adjunctive therapy in acute, painful musculoskeletal conditions. "( Abuse potential of carisoprodol: a retrospective review of Idaho Medicaid pharmacy and medical claims data.
Cady, P; Culbertson, V; Force, R; Owens, C; Pugmire, B; Salness, T; Steiner, J, 2007
)
2.11
"Carisoprodol is a drug frequently prescribed for lower back pain. "( Acute intoxications with carisoprodol.
Bramness, J; Høiseth, G; Sørlid, HK, 2008
)
2.09
"Carisoprodol is a muscle relaxant analgesic, which has an active metabolite i.e. "( Formation of meprobamate from carisoprodol is catalysed by CYP2C19.
Alvan, G; Dalén, P; Olsen, H; Wakelkamp, M, 1996
)
2.03
"Carisoprodol (Soma) is a noncontrolled, skeletal-muscle relaxant whose active metabolite is meprobamate. "( Carisoprodol: a drug of continuing abuse.
Carter, OS; Pinkofsky, HB; Reeves, RR, 1997
)
3.18
"Carisoprodol is a skeletal muscle relaxant with the potential for abuse. "( A review of carisoprodol deaths in Jefferson County, Alabama.
Alexander, CB; Davis, GG, 1998
)
2.12
"Carisoprodol is a noncontrolled skeletal muscle relaxant whose active metabolite is meprobamate, a Schedule IV controlled substance. "( Carisoprodol (soma): abuse potential and physician unawareness.
Bennett, DM; Carter, OS; Pinkofsky, HB; Reeves, RR; Struve, FA, 1999
)
3.19

Effects

Carisoprodol probably has an impairing effect by itself, at least at blood concentration levels above which can be seen after therapeutic intake of the drug. Carisoprodol has a short elimination half-life of 1-3 h; however, its major active metabolite, meprobamate, has a longer elimination half life of 6-17 h.

Carisoprodol has a short elimination half-life of 1-3 h. It has been classified as a controlled substance in several states in the US. Restrictions on the use of the drug have been imposed in some European countries.

ExcerptReferenceRelevance
"Carisoprodol has a short elimination half-life of 1-3 h; however, its major active metabolite, meprobamate, has a longer elimination half-life of 6-17 h."( Validation of a new homogeneous immunoassay for the detection of carisoprodol in urine.
Barhate, R; Coulter, C; Huynh, K; Moore, C; Rodrigues, W; Soares, J; Vincent, M; Wang, G, 2011
)
1.33
"Carisoprodol probably has an impairing effect by itself, at least at blood concentration levels above which can be seen after therapeutic intake of the drug."( Impairment due to intake of carisoprodol.
Bramness, JG; Mørland, J; Skurtveit, S, 2004
)
2.06
"Carisoprodol has been classified as a controlled substance in several states in the US and restrictions on the use of the drug have been imposed in some European countries."( Carisoprodol: abuse potential and withdrawal syndrome.
Burke, RS; Reeves, RR, 2010
)
2.52
"Carisoprodol has a short elimination half-life of 1-3 h; however, its major active metabolite, meprobamate, has a longer elimination half-life of 6-17 h."( Validation of a new homogeneous immunoassay for the detection of carisoprodol in urine.
Barhate, R; Coulter, C; Huynh, K; Moore, C; Rodrigues, W; Soares, J; Vincent, M; Wang, G, 2011
)
1.33
"Carisoprodol probably has an impairing effect by itself, at least at blood concentration levels above which can be seen after therapeutic intake of the drug."( Impairment due to intake of carisoprodol.
Bramness, JG; Mørland, J; Skurtveit, S, 2004
)
2.06

Treatment

Carisoprodol treatment resulted in tolerance and antagonist-precipitated withdrawal, suggesting it may have an addiction potential similar to that of other long-acting benzodiazepine or barbiturate compounds. Treatment with carisoprodol and phenobarbital provided additional benefit and can be considered in cases of severe carisobrodol withdrawal.

ExcerptReferenceRelevance
"Carisoprodol treatment resulted in tolerance and antagonist-precipitated withdrawal, suggesting it may have an addiction potential similar to that of other long-acting benzodiazepine or barbiturate compounds."( Carisoprodol tolerance and precipitated withdrawal.
Carbonaro, T; Forster, MJ; Gatch, MB; Nguyen, JD, 2012
)
3.26
"Treatment with carisoprodol and phenobarbital provided additional benefit and can be considered in cases of severe carisoprodol withdrawal."( Severe Carisoprodol Withdrawal After a 14-Year Addiction and Acute Overdose.
Benowitz, NL; Horng, H; Smollin, CG; Vo, KT, 2017
)
1.25

Pharmacokinetics

A two-compartment pharmacokinetic model describing carisoprodol metabolism and that of the primary metabolite, meprobamate, was developed to better understand the pharmacokinetics of this drug. No significant differences with respect to the CYP2C19 IM and EM genotypes were observed in the acute impairing effects of a single dose of carisobrodol.

ExcerptReferenceRelevance
" During this time period, different pharmacodynamic measurements were made."( The CYP2C19 genotype and the use of oral contraceptives influence the pharmacokinetics of carisoprodol in healthy human subjects.
Bramness, JG; Breilid, H; Gulliksen, M; Mørland, J; Skurtveit, S; Steen, VM, 2005
)
0.55
" No significant differences in pharmacodynamic parameters were found between subjects in the different genotype groups or between users and non-users of oral contraceptives."( The CYP2C19 genotype and the use of oral contraceptives influence the pharmacokinetics of carisoprodol in healthy human subjects.
Bramness, JG; Breilid, H; Gulliksen, M; Mørland, J; Skurtveit, S; Steen, VM, 2005
)
0.55
" Despite these pharmacokinetic effects, no significant differences with respect to the CYP2C19 IM and EM genotypes were observed in the acute impairing effects of a single dose of carisoprodol."( The CYP2C19 genotype and the use of oral contraceptives influence the pharmacokinetics of carisoprodol in healthy human subjects.
Bramness, JG; Breilid, H; Gulliksen, M; Mørland, J; Skurtveit, S; Steen, VM, 2005
)
0.74
" The validated method was successfully applied to a pharmacokinetic study following co-administration of carisoprodol (250 mg) and aspirin (75 mg) tablets by oral route to human volunteers."( Simultaneous determination of carisoprodol and aspirin in human plasma using liquid chromatography-tandem mass spectrometry in polarity switch mode: application to a human pharmacokinetic study.
Babu, RV; Krishnaiah, A; Kumar, IJ; Pilli, NR; Ramesh, M; Sreenivasulu, V, 2013
)
0.89
" A two-compartment pharmacokinetic model describing carisoprodol metabolism and that of the primary metabolite, meprobamate, was developed to better understand the pharmacokinetics of this drug."( Pharmacokinetic modeling of carisoprodol and meprobamate disposition in adults.
Lewandowski, TA, 2017
)
1

Compound-Compound Interactions

ExcerptReferenceRelevance
"This hypothesis was tested in an experiment where information about the effect of a drug was combined with administration of an active drug or placebo."( Stimulant and relaxant drugs combined with stimulant and relaxant information: a study of active placebo.
Aamo, T; Flaten, MA; Olsen, H; Sager, G; Simonsen, T; Zahlsen, K, 2004
)
0.32

Bioavailability

ExcerptReferenceRelevance
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

The objective of this placebo-controlled trial was to determine the efficacy and safety of carisoprodol (Soma, MedPointe Pharmaceuticals, Somerset, NJ, USA) The drug is a centrally acting skeletal muscle relaxant used to treat acute, painful musculoskeletal conditions.

ExcerptRelevanceReference
" This result indicates a gene dosage effect where the carisoprodol : meprobamate ratio reflects the number of active CYP2C19 alleles."( Association between blood carisoprodol:meprobamate concentration ratios and CYP2C19 genotype in carisoprodol-drugged drivers: decreased metabolic capacity in heterozygous CYP2C19*1/CYP2C19*2 subjects?
Bramness, JG; Fauske, L; Grung, M; Molven, A; Mørland, J; Skurtveit, S; Steen, VM, 2003
)
0.87
"The objective of this placebo-controlled trial was to determine the efficacy and safety of carisoprodol (Soma, MedPointe Pharmaceuticals, Somerset, NJ, USA), a centrally acting skeletal muscle relaxant used to treat acute, painful musculoskeletal conditions, at a dosage of 250 mg three times daily and at bedtime in patients with acute, painful muscle spasm of the lower back."( Double-blind, placebo-controlled trial of carisoprodol 250-mg tablets in the treatment of acute lower-back spasm.
Look, M; Ralph, L; Sacks, H; Wheeler, W, 2008
)
0.83
" This study has been conducted to clarify the treatment with a high and low dosage of carisoprodol (Somadril) on the histopathological, histochemical changes in the fetal ileum of the Albino rats."( Toxicity of Somadril Compound on Fetal Ileum Tissues of Albino Rats.
Ahmed Abd Rabou, M; Alhumaidi Alotaibi, M, 2021
)
0.84
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (1)

RoleDescription
muscle relaxantA drug used to produce muscle relaxation (excepting neuromuscular blocking agents). Its primary clinical and therapeutic use is the treatment of muscle spasm and immobility associated with strains, sprains, and injuries of the back and, to a lesser degree, injuries to the neck. Also used for the treatment of a variety of clinical conditions that have in common only the presence of skeletal muscle hyperactivity, for example, the muscle spasms that can occur in multiple sclerosis.
[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 (1)

ClassDescription
carbamate esterAny ester of carbamic acid or its N-substituted derivatives.
[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 (39)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, TYROSYL-DNA PHOSPHODIESTERASEHomo sapiens (human)Potency0.79430.004023.8416100.0000AID485290
thioredoxin reductaseRattus norvegicus (Norway rat)Potency29.93490.100020.879379.4328AID588453
RAR-related orphan receptor gammaMus musculus (house mouse)Potency76.72410.006038.004119,952.5996AID1159521
USP1 protein, partialHomo sapiens (human)Potency0.00840.031637.5844354.8130AID504865
NFKB1 protein, partialHomo sapiens (human)Potency14.12540.02827.055915.8489AID895; AID928
thyroid stimulating hormone receptorHomo sapiens (human)Potency0.63100.001318.074339.8107AID926; AID938
EWS/FLI fusion proteinHomo sapiens (human)Potency0.01050.001310.157742.8575AID1259252
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency26.83250.000214.376460.0339AID720692
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency47.52410.003041.611522,387.1992AID1159552; AID1159555
pregnane X nuclear receptorHomo sapiens (human)Potency35.48130.005428.02631,258.9301AID720659
estrogen nuclear receptor alphaHomo sapiens (human)Potency34.20430.000229.305416,493.5996AID588513; AID743080
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency0.35480.035520.977089.1251AID504332
chromobox protein homolog 1Homo sapiens (human)Potency0.00600.006026.168889.1251AID488953
flap endonuclease 1Homo sapiens (human)Potency8.43680.133725.412989.1251AID588795
ras-related protein Rab-9AHomo sapiens (human)Potency6.30960.00022.621531.4954AID485297
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency89.12510.050127.073689.1251AID588590
gemininHomo sapiens (human)Potency1.25890.004611.374133.4983AID624297
DNA polymerase kappa isoform 1Homo sapiens (human)Potency35.48130.031622.3146100.0000AID588579
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency12.58930.031610.279239.8107AID884; AID885
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency0.10000.00106.000935.4813AID943
lamin isoform A-delta10Homo sapiens (human)Potency0.00560.891312.067628.1838AID1487
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency12.58931.000012.224831.6228AID885
Rap guanine nucleotide exchange factor 3Homo sapiens (human)Potency35.48136.309660.2008112.2020AID720707
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency12.58931.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency12.58931.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency12.58931.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency12.58931.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency12.58931.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency12.58931.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency12.58931.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency12.58931.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency12.58931.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency12.58931.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency12.58931.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency12.58931.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency12.58931.000012.224831.6228AID885
GABA theta subunitRattus norvegicus (Norway rat)Potency12.58931.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency12.58931.000012.224831.6228AID885
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency16.94410.060110.745337.9330AID485368
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (20)

Processvia Protein(s)Taxonomy
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)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (4)

Processvia Protein(s)Taxonomy
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)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (8)

Processvia Protein(s)Taxonomy
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)
plasma membraneGamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (117)

Assay IDTitleYearJournalArticle
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID1745845Primary qHTS for Inhibitors of ATXN expression
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.
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.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation 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.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation 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.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation 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.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation 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.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation 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.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation 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.
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.
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.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
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.
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.
AID588378qHTS for Inhibitors of ATXN expression: Validation
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.
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.
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.
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.
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]
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.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' 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).
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).
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]
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID395325Lipophilicity, log P by microemulsion electrokinetic chromatography2009Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
Relationship between brain tissue partitioning and microemulsion retention factors of CNS drugs.
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.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID106806Inhibition of malate dehydrogenase (MDH) at 400 uM2003Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21
Identification and prediction of promiscuous aggregating inhibitors among known drugs.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
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).
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
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.
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).
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
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]
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.
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
AID468443Inhibition of human FAAH at 1 uM2009Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23
Mining biologically-active molecules for inhibitors of fatty acid amide hydrolase (FAAH): identification of phenmedipham and amperozide as FAAH inhibitors.
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.
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).
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID52790Inhibition of chymotrypsin at 250 uM2003Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21
Identification and prediction of promiscuous aggregating inhibitors among known 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).
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).
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).
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID43581Inhibition of beta-lactamase at 100 uM2003Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21
Identification and prediction of promiscuous aggregating inhibitors among known drugs.
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]
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.
AID1215127Ratio of fraction unbound in solid supported porcine brain membrane vesicles at 5 uM by TRANSIL assay to fraction unbound in Wistar rat brain homogenate at 5 uM after 5 hrs by equilibrium dialysis method2011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Brain tissue binding of drugs: evaluation and validation of solid supported porcine brain membrane vesicles (TRANSIL) as a novel high-throughput method.
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).
AID395324Lipophilicity, log D at pH 7.4 by liquid chromatography2009Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
Relationship between brain tissue partitioning and microemulsion retention factors of CNS drugs.
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).
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.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID1215122Percentage unbound in solid supported porcine brain membrane vesicles at 5 uM by TRANSIL assay2011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Brain tissue binding of drugs: evaluation and validation of solid supported porcine brain membrane vesicles (TRANSIL) as a novel high-throughput method.
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]
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).
AID1215121Fraction unbound in Wistar rat brain homogenate at 5 uM after 5 hrs by equilibrium dialysis method2011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Brain tissue binding of drugs: evaluation and validation of solid supported porcine brain membrane vesicles (TRANSIL) as a novel high-throughput method.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' 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).
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).
AID298031Lipophilicity, log D at pH7.42007Journal of medicinal chemistry, Sep-20, Volume: 50, Issue:19
High-throughput screening of drug-brain tissue binding and in silico prediction for assessment of central nervous system drug delivery.
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).
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.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
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.
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.
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.
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.
AID1224864HCS microscopy assay (F508del-CFTR)2016PloS one, , Volume: 11, Issue:10
Increasing the Endoplasmic Reticulum Pool of the F508del Allele of the Cystic Fibrosis Transmembrane Conductance Regulator Leads to Greater Folding Correction by Small Molecule Therapeutics.
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.
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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (393)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990215 (54.71)18.7374
1990's25 (6.36)18.2507
2000's65 (16.54)29.6817
2010's69 (17.56)24.3611
2020's19 (4.83)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 98.02

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 Index98.02 (24.57)
Research Supply Index6.11 (2.92)
Research Growth Index4.60 (4.65)
Search Engine Demand Index178.12 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (98.02)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials22 (5.16%)5.53%
Reviews20 (4.69%)6.00%
Case Studies39 (9.15%)4.05%
Observational0 (0.00%)0.25%
Other345 (80.99%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (3)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
A Phase 1/2a, Controlled, Randomized, Multicenter Study Evaluating the Efficacy, Safety, and Tolerability of StrataGraft Overlay of Meshed Autograft (SOMA) in Treatment of Full-Thickness Thermal Burns [NCT04765202]Phase 240 participants (Anticipated)Interventional2021-05-28Recruiting
Randomized, Double-Blind, Double-Dummy Trial of Two Sustained Release Formulations of Carisoprodol Compared to Placebo in Subjects With Acute, Painful, Musculoskeletal Spasm of the Lower Back [NCT00671879]Phase 3830 participants (Actual)Interventional2008-04-30Completed
Randomized, Double-Blind, Double-Dummy Trial of Two Sustained Release Formulations of Carisoprodol Compared to Placebo in Subjects With Acute, Painful, Musculoskeletal Spasm of the Lower Back [NCT00671502]Phase 3840 participants (Actual)Interventional2008-04-30Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00671502 (1) [back to overview]Subject Rating of Pain on a 100-point Visual Analog Scale (VAS)
NCT00671879 (2) [back to overview]Subject Functional Assessment Based on the Roland-Morris Disability Questionnaire (RMDQ)
NCT00671879 (2) [back to overview]Subject Rated Change Relief From Starting Backache of Pain on a 100-point Visual Analog Scale

Subject Rating of Pain on a 100-point Visual Analog Scale (VAS)

the scale used was from 0 to 100 mm. 0 equaled no pain and 100 equaled maximum pain.participants measure their pain before treatment and during treatment at each visit (NCT00671502)
Timeframe: up to 14 days

Interventionmm (Least Squares Mean)
Carisoprodol 500mg Tablets27.5
Carisoprodol 700mg Tablets28
Placebo Tablets28.6

[back to top]

Subject Functional Assessment Based on the Roland-Morris Disability Questionnaire (RMDQ)

Subject functional assessment based on the Roland-Morris Disability Questionnaire (RMDQ)at day 14.Subjects were asked to read a list of 24 sentences that people have used to describe themselves when they had back pain, and were asked to mark those statements that described their condition that day. The number of marked statements was added. A decrease in the number of marked statements from baseline represented improvement on the RMDQ. (NCT00671879)
Timeframe: baseline and day +14

Interventionmarked statements (Least Squares Mean)
Carisprodol SR 700 mg4.2
Carisoprodol SR 500mg5.0
Placebo4.3

[back to top]

Subject Rated Change Relief From Starting Backache of Pain on a 100-point Visual Analog Scale

on a visual analog scale of 0 to 100 millimeters(mm) with 0 being no pain and 100 being maximum pain By measuring the amount of pain before and during treatment done at each visit and recording the difference in mm.During treatment scores were averaged and this average was compared to the baseline value. (NCT00671879)
Timeframe: baseline to 14 days

Interventionmm (Least Squares Mean)
Carisprodol SR 700 mg16.4
Carisoprodol SR 500mg15.5
Placebo15.2

[back to top]