phenobarbital sodium profile

2-(phosphonomethyl)pentanedioic acid: an N-acetylated alpha-linked acidic dipeptidase (NAALADase) antagonist [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

ID Source	ID
PubMed CID	23674889
CHEMBL ID	149972
CHEBI ID	8070
SCHEMBL ID	42037
MeSH ID	M0331275
PubMed CID	10130754
CHEMBL ID	47009
SCHEMBL ID	383173
MeSH ID	M0331275

Synonym
sodium 5-ethyl-4,6-dioxo-5-phenyl-1,4,5,6-tetrahydropyrimidin-2-olate
phenobarbital, sodium
phenobarbital, monosodium salt
phenobarbitone sodium
phenobarbitalnatrium
phenobarbitone sodium salt
barbituric acid, 5-ethyl-5-phenyl-, sodium salt
soluble phenobarbital
sodium ethylphenylbarbiturate
phenobarbital elixir
phenemalnatrium
5-ethyl-5-phenyl-2,4,6-(1h,3h,5h)pyrimidinetrione monosodium salt
sol phenobarbital
fenobarbital sodico [inn-spanish]
sodium phenylethylmalonyurea
phenobarbitalum natricum [inn-latin]
gardenal sodium
phenobarbiton-natrium
ccris 503
sol phenobarbitone
phenobarbital na
soluble phenobarbitone
phenobarbital sodique [inn-french]
fenobarbital natrium [polish]
phenobal sodium
einecs 200-322-3
phenyl-aethyl-barbitursaeure natrium [german]
phenylethylbarbituric acid, sodium salt
sodium, phenobarbital
monosodium salt phenobarbital
phenobarbital sodium salt
57-30-7
phenobarbital sodium (jan/usp/inn)
D00701
luminal sodium (tn)
5-ethyl-5-phenylbarbituric acid sodium salt
phenobarbitalum natricum
phenyl-aethyl-barbitursaeure natrium
sodium phenobarbiturate
sodium phenylethylmalonylurea
phenobarbital sodium ,
CHEBI:8070 ,
sodium phenobarbitone
luminal sodium
sodium 5-ethyl-5-phenylbarbiturate
sodium phenobarbital
sodium phenylethylbarbiturate
sodium luminal
phenobarbital sodique
AC-11674
CHEMBL149972
phenobarbital sod
A831383
sodium 5-ethyl-4,6-bis(oxidanylidene)-5-phenyl-1h-pyrimidin-2-olate
sodium 5-ethyl-4,6-dioxo-5-phenyl-1h-pyrimidin-2-olate
dtxsid0021123 ,
dtxcid101123
tox21_300271
cas-57-30-7
NCGC00253999-01
P0890
AKOS015960550
sw9m9bb5k3 ,
phenobarbital sodium [usp:inn:jan]
unii-sw9m9bb5k3
fenobarbital sodico
fenobarbital natrium
SCHEMBL42037
WRLGYAWRGXKSKG-UHFFFAOYSA-M
W-105476
5-ethyl-5-phenyl-2,4,6(1h,3h,5h)-pyrimidinetrione sodium salt
Q26840934
sodium;5-ethyl-4,6-dioxo-5-phenyl-1h-pyrimidin-2-olate
sodium;5-ethyl-5-phenylpyrimidin-3-ide-2,4,6-trione
phenobarbital sodium (usp:inn:jan)
5-ethyl-5-phenylbarbituric acid sodium
phenobarbital sodique (inn-french)
barbituric acid, 5-ethyl-5-phenyl, sodium salt
phenobarbital sodium (mart.)
fenobarbital sodico (inn-spanish)
phenobarbital sodium (usp monograph)
phenobarbital sodium (ep monograph)
phenobarbitalum natricum (inn-latin)
HMS3267D10
NCGC00167723-01
(r,s)-2-phosphonomethylpentanedioic acid
2-(phosphonomethyl)pentanedioic acid
2-pmpa
chembl47009 ,
bdbm17659
2-phosphonomethyl-pentanedioic acid
173039-10-6
pentanedioic acid, 2-(phosphonomethyl)-
AKOS016004257
2-(phosphonomethyl)-pentanedioic acid
SCHEMBL383173
pmpa (naaladase inhibitor)
2-(phosphonomethyl)pentane-1,5-dioic acid
DTXSID90436036
HY-100788
CS-6202
pmpa(naaladaseinhibitor)
EX-A1248
2-pmpa, >=98% (hplc)
J-010872
2-pmpa(naaladaseinhibitor)
pmpa free acid
173039-10-6 (free acid)
ISEYJGQFXSTPMQ-UHFFFAOYSA-N
HMS3676K10
HMS3412K10
2-(phosphonomethyl)pentanedioic acid (pmpa)
mfcd00940167
HMS3749M13
YGA03910
unii-xh88wjg9lj
xh88wjg9lj ,

Excerpt	Reference	Relevance
" We report that, at high concentrations (300 microM-30 mM), a folic acid hexaglutamate analog is dose-dependently toxic to dissociated rat cortical cultures and that this toxicity is reversed by 2-PMPA, a potent and selective NAALADase inhibitor."	( Toxicity induced by a polyglutamated folate analog is attenuated by NAALADase inhibition. Olkowski, JL; Slusher, BS; Thomas, AG; Vornov, JJ, 1999)	0.3

Excerpt	Reference	Relevance
" The purpose of this study was to develop a pharmacodynamic (PD) marker assay to use in clinical development."	( Glutamate carboxypeptidase activity in human skin biopsies as a pharmacodynamic marker for clinical studies. Ebenezer, GJ; Polydefkis, M; Rojas, C; Rudek, MA; Slusher, BS; Stathis, M; Zhao, M, 2011)	0.37

Excerpt	Reference	Relevance
" The most potent thiol-based inhibitor, 2-(3-mercaptopropyl)pentanedioic acid (IC(50) = 90 nM), was found to be orally bioavailable in rats and exhibited efficacy in an animal model of neuropathic pain following oral administration."	( Synthesis and biological evaluation of thiol-based inhibitors of glutamate carboxypeptidase II: discovery of an orally active GCP II inhibitor. Burak, E; Delahanty, G; Grella, BS; Jackson, PF; Ko, YS; Li, W; Limsakun, T; Liu, Q; Maclin, KM; Majer, P; Poláková, J; Rojas, C; Shaffer, KA; Slusher, BS; Stoermer, D; Tsukamoto, T; Vitharana, D; Wang, EY; Wozniak, KM; Zakrzewski, A, 2003)	0.32
" In addition, E2072 was found to be orally available with an absolute bioavailability of ∼30% in rats and ∼39% in monkeys."	( Reversible disulfide formation of the glutamate carboxypeptidase II inhibitor E2072 results in prolonged systemic exposures in vivo. Alt, J; Hoover, R; Rais, R; Rojas, C; Rudek, MA; Slusher, BS; Tsukamoto, T; Wozniak, K, 2012)	0.38
" Unfortunately no GCP-II inhibitor has advanced clinically, largely due to their highly polar nature resulting in insufficient oral bioavailability and limited brain penetration."	( Selective CNS Uptake of the GCP-II Inhibitor 2-PMPA following Intranasal Administration. Alt, J; Giroux, M; Niwa, M; Rais, R; Rojas, C; Sawa, A; Slusher, BS; Stathis, M; Wozniak, K; Wu, Y, 2015)	0.42

Excerpt	Relevance	Reference
" Linear regression analysis of dose-response relationship between the doses of 2-PMPA and their corresponding threshold values allowed the calculation of threshold increasing dose by 20% (TID20), which was 109."	( 2-phosphonomethyl-pentanedioic acid (glutamate carboxypeptidase II inhibitor) increases threshold for electroconvulsions and enhances the antiseizure action of valproate against maximal electroshock-induced seizures in mice. Czuczwar, SJ; Luszczki, JJ; Mohamed, M, 2006)	0.33
" Inhibition of the neuropeptidase glutamate carboxypeptidase II (GCPII) has previously been shown to ameliorate cognitive impairment in EAE, but dosing has not yet been optimized and only a prevention treatment paradigm has been explored."	( Dose-dependent inhibition of GCPII to prevent and treat cognitive impairment in the EAE model of multiple sclerosis. Alt, J; Hollinger, KR; Kaplin, AI; Riehm, AM; Slusher, BS, 2016)	0.43

Class	Description
organic sodium salt
barbiturates	Members of the class of pyrimidones consisting of pyrimidine-2,4,6(1H,3H,5H)-trione (barbituric acid) and its derivatives. Largest group of the synthetic sedative/hypnotics, sharing a characteristic six-membered ring structure.
[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	Taxonomy	Measurement	Average (µ)	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
retinoic acid nuclear receptor alpha variant 1	Homo sapiens (human)	Potency	41.4374	0.0030	41.6115	22,387.1992	AID1159552; AID1159555
retinoid X nuclear receptor alpha	Homo sapiens (human)	Potency	14.4474	0.0008	17.5051	59.3239	AID1159527; AID1159531
pregnane X nuclear receptor	Homo sapiens (human)	Potency	53.0453	0.0054	28.0263	1,258.9301	AID1346982
thyroid hormone receptor beta isoform 2	Rattus norvegicus (Norway rat)	Potency	74.9285	0.0003	23.4451	159.6830	AID743066
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Cytochrome P450 3A4	Homo sapiens (human)	IC50 (µMol)	0.0011	0.0001	1.7536	10.0000	AID705577
Cytochrome P450 3A4	Homo sapiens (human)	Ki	0.0004	0.0001	1.4162	9.9000	AID705577; AID705578
Cytochrome P450 2C9	Homo sapiens (human)	Ki	0.0003	0.0003	1.6842	10.0000	AID705578
Cytochrome P450 2B6	Homo sapiens (human)	IC50 (µMol)	0.0011	0.0011	3.4186	10.0000	AID705577
Cytochrome P450 2B6	Homo sapiens (human)	Ki	0.0004	0.0004	1.4160	10.0000	AID705577
Glutamate carboxypeptidase 2	Rattus norvegicus (Norway rat)	IC50 (µMol)	0.0027	0.0003	0.7889	2.4000	AID143897; AID74536
Glutamate carboxypeptidase 2	Rattus norvegicus (Norway rat)	Ki	0.0003	0.0003	0.0003	0.0003	AID71198
Glutamate carboxypeptidase 2	Homo sapiens (human)	IC50 (µMol)	0.0196	0.0003	0.8316	9.5000	AID1210717; AID1290367; AID1797641; AID1797656; AID1797657; AID1846365; AID1876792; AID315181; AID705577; AID74530; AID74531
Glutamate carboxypeptidase 2	Homo sapiens (human)	Ki	0.0054	0.0002	0.0046	0.0312	AID1226540; AID705577; AID705578; AID74532; AID74533; AID773968
N-acetylated-alpha-linked acidic dipeptidase 2	Homo sapiens (human)	Ki	0.0014	0.0014	0.0014	0.0014	AID74534
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Glutamate carboxypeptidase 2	Homo sapiens (human)	EC50 (µMol)	0.0006	0.0006	0.0068	0.0130	AID74529
Glutamate carboxypeptidase 2	Homo sapiens (human)	Kd	0.0005	0.0004	0.0005	0.0005	AID411794; AID411795
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Process	via Protein(s)	Taxonomy
lipid hydroxylation	Cytochrome P450 3A4	Homo sapiens (human)
lipid metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
steroid catabolic process	Cytochrome P450 3A4	Homo sapiens (human)
xenobiotic metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
steroid metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
cholesterol metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
androgen metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
estrogen metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
alkaloid catabolic process	Cytochrome P450 3A4	Homo sapiens (human)
monoterpenoid metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
calcitriol biosynthetic process from calciol	Cytochrome P450 3A4	Homo sapiens (human)
xenobiotic catabolic process	Cytochrome P450 3A4	Homo sapiens (human)
vitamin D metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
vitamin D catabolic process	Cytochrome P450 3A4	Homo sapiens (human)
retinol metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
retinoic acid metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
long-chain fatty acid biosynthetic process	Cytochrome P450 3A4	Homo sapiens (human)
aflatoxin metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
oxidative demethylation	Cytochrome P450 3A4	Homo sapiens (human)
xenobiotic metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
steroid metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
cholesterol metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
estrogen metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
monoterpenoid metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
epoxygenase P450 pathway	Cytochrome P450 2C9	Homo sapiens (human)
urea metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
monocarboxylic acid metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
xenobiotic catabolic process	Cytochrome P450 2C9	Homo sapiens (human)
long-chain fatty acid biosynthetic process	Cytochrome P450 2C9	Homo sapiens (human)
amide metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
icosanoid biosynthetic process	Cytochrome P450 2C9	Homo sapiens (human)
oxidative demethylation	Cytochrome P450 2C9	Homo sapiens (human)
omega-hydroxylase P450 pathway	Cytochrome P450 2C9	Homo sapiens (human)
xenobiotic metabolic process	Cytochrome P450 2B6	Homo sapiens (human)
steroid metabolic process	Cytochrome P450 2B6	Homo sapiens (human)
xenobiotic catabolic process	Cytochrome P450 2B6	Homo sapiens (human)
cellular ketone metabolic process	Cytochrome P450 2B6	Homo sapiens (human)
epoxygenase P450 pathway	Cytochrome P450 2B6	Homo sapiens (human)
proteolysis	Glutamate carboxypeptidase 2	Homo sapiens (human)
folic acid-containing compound metabolic process	Glutamate carboxypeptidase 2	Homo sapiens (human)
C-terminal protein deglutamylation	Glutamate carboxypeptidase 2	Homo sapiens (human)
proteolysis	N-acetylated-alpha-linked acidic dipeptidase 2	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
monooxygenase activity	Cytochrome P450 3A4	Homo sapiens (human)
steroid binding	Cytochrome P450 3A4	Homo sapiens (human)
iron ion binding	Cytochrome P450 3A4	Homo sapiens (human)
protein binding	Cytochrome P450 3A4	Homo sapiens (human)
steroid hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
retinoic acid 4-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
oxidoreductase activity	Cytochrome P450 3A4	Homo sapiens (human)
oxygen binding	Cytochrome P450 3A4	Homo sapiens (human)
enzyme binding	Cytochrome P450 3A4	Homo sapiens (human)
heme binding	Cytochrome P450 3A4	Homo sapiens (human)
vitamin D3 25-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
caffeine oxidase activity	Cytochrome P450 3A4	Homo sapiens (human)
quinine 3-monooxygenase activity	Cytochrome P450 3A4	Homo sapiens (human)
testosterone 6-beta-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
1-alpha,25-dihydroxyvitamin D3 23-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
anandamide 8,9 epoxidase activity	Cytochrome P450 3A4	Homo sapiens (human)
anandamide 11,12 epoxidase activity	Cytochrome P450 3A4	Homo sapiens (human)
anandamide 14,15 epoxidase activity	Cytochrome P450 3A4	Homo sapiens (human)
aromatase activity	Cytochrome P450 3A4	Homo sapiens (human)
vitamin D 24-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
estrogen 16-alpha-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
estrogen 2-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
1,8-cineole 2-exo-monooxygenase activity	Cytochrome P450 3A4	Homo sapiens (human)
monooxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
iron ion binding	Cytochrome P450 2C9	Homo sapiens (human)
arachidonic acid epoxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
steroid hydroxylase activity	Cytochrome P450 2C9	Homo sapiens (human)
arachidonic acid 14,15-epoxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
arachidonic acid 11,12-epoxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
oxidoreductase activity	Cytochrome P450 2C9	Homo sapiens (human)
(S)-limonene 6-monooxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
(S)-limonene 7-monooxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
caffeine oxidase activity	Cytochrome P450 2C9	Homo sapiens (human)
(R)-limonene 6-monooxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
aromatase activity	Cytochrome P450 2C9	Homo sapiens (human)
heme binding	Cytochrome P450 2C9	Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen	Cytochrome P450 2C9	Homo sapiens (human)
monooxygenase activity	Cytochrome P450 2B6	Homo sapiens (human)
iron ion binding	Cytochrome P450 2B6	Homo sapiens (human)
testosterone 16-alpha-hydroxylase activity	Cytochrome P450 2B6	Homo sapiens (human)
heme binding	Cytochrome P450 2B6	Homo sapiens (human)
testosterone 16-beta-hydroxylase activity	Cytochrome P450 2B6	Homo sapiens (human)
anandamide 8,9 epoxidase activity	Cytochrome P450 2B6	Homo sapiens (human)
anandamide 11,12 epoxidase activity	Cytochrome P450 2B6	Homo sapiens (human)
anandamide 14,15 epoxidase activity	Cytochrome P450 2B6	Homo sapiens (human)
estrogen 2-hydroxylase activity	Cytochrome P450 2B6	Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen	Cytochrome P450 2B6	Homo sapiens (human)
arachidonic acid epoxygenase activity	Cytochrome P450 2B6	Homo sapiens (human)
metallocarboxypeptidase activity	Glutamate carboxypeptidase 2	Homo sapiens (human)
peptidase activity	Glutamate carboxypeptidase 2	Homo sapiens (human)
dipeptidase activity	Glutamate carboxypeptidase 2	Homo sapiens (human)
metal ion binding	Glutamate carboxypeptidase 2	Homo sapiens (human)
Ac-Asp-Glu binding	Glutamate carboxypeptidase 2	Homo sapiens (human)
tetrahydrofolyl-poly(glutamate) polymer binding	Glutamate carboxypeptidase 2	Homo sapiens (human)
carboxypeptidase activity	Glutamate carboxypeptidase 2	Homo sapiens (human)
carboxypeptidase activity	N-acetylated-alpha-linked acidic dipeptidase 2	Homo sapiens (human)
metallocarboxypeptidase activity	N-acetylated-alpha-linked acidic dipeptidase 2	Homo sapiens (human)
protein binding	N-acetylated-alpha-linked acidic dipeptidase 2	Homo sapiens (human)
serine-type peptidase activity	N-acetylated-alpha-linked acidic dipeptidase 2	Homo sapiens (human)
dipeptidyl-peptidase activity	N-acetylated-alpha-linked acidic dipeptidase 2	Homo sapiens (human)
dipeptidase activity	N-acetylated-alpha-linked acidic dipeptidase 2	Homo sapiens (human)
metal ion binding	N-acetylated-alpha-linked acidic dipeptidase 2	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
cytoplasm	Cytochrome P450 3A4	Homo sapiens (human)
endoplasmic reticulum membrane	Cytochrome P450 3A4	Homo sapiens (human)
intracellular membrane-bounded organelle	Cytochrome P450 3A4	Homo sapiens (human)
endoplasmic reticulum membrane	Cytochrome P450 2C9	Homo sapiens (human)
plasma membrane	Cytochrome P450 2C9	Homo sapiens (human)
intracellular membrane-bounded organelle	Cytochrome P450 2C9	Homo sapiens (human)
cytoplasm	Cytochrome P450 2C9	Homo sapiens (human)
intracellular membrane-bounded organelle	Cytochrome P450 2C9	Homo sapiens (human)
endoplasmic reticulum membrane	Cytochrome P450 2B6	Homo sapiens (human)
intracellular membrane-bounded organelle	Cytochrome P450 2B6	Homo sapiens (human)
cytoplasm	Cytochrome P450 2B6	Homo sapiens (human)
cytoplasm	Glutamate carboxypeptidase 2	Homo sapiens (human)
plasma membrane	Glutamate carboxypeptidase 2	Homo sapiens (human)
cell surface	Glutamate carboxypeptidase 2	Homo sapiens (human)
membrane	Glutamate carboxypeptidase 2	Homo sapiens (human)
extracellular exosome	Glutamate carboxypeptidase 2	Homo sapiens (human)
plasma membrane	Glutamate carboxypeptidase 2	Homo sapiens (human)
plasma membrane	N-acetylated-alpha-linked acidic dipeptidase 2	Homo sapiens (human)
membrane	N-acetylated-alpha-linked acidic dipeptidase 2	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (77)

Assay ID	Title	Year	Journal	Article
AID1145213	Anticonvulsant activity in mouse assessed as protection against maximal electroshock-induced seizures	1976	Journal of medicinal chemistry, Mar, Volume: 19, Issue:3	Synthesis and central nervous system depressant activity of some bicyclic amides.
AID1149324	Behavioral toxicity in po dosed albino Icem-CET (SPF Caw) mouse assessed as tremors by Irwin's test	1977	Journal of medicinal chemistry, Jan, Volume: 20, Issue:1	Structure-activity relationship in cinnamamides. 2. Synthesis and pharmacological evaluation of some (E)- and (Z)-N-alkyl-alpha, beta-dimethylcinnamamides substituted on the phenyl group.
AID1145217	Reinduction of anesthesia-induced loss of righting in dosed mouse administered compound following recovery from hexobarbital anesthesia	1976	Journal of medicinal chemistry, Mar, Volume: 19, Issue:3	Synthesis and central nervous system depressant activity of some bicyclic amides.
AID1129992	Anticonvulsant activity in Swiss Webster mouse assessed as PTZ-induced tonic seizures at 30 mg/kg, ip pretreated 20 mins before PTZ challenge and measured 1 hr post PTZ challenge relative to control	2014	Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7	Synthesis and anticonvulsant activity of some new pyrazolo[3,4-b]pyrazines and related heterocycles.
AID1149325	Behavioral toxicity in po dosed albino Icem-CET (SPF Caw) mouse measured up to 7 days by Irwin's test	1977	Journal of medicinal chemistry, Jan, Volume: 20, Issue:1	Structure-activity relationship in cinnamamides. 2. Synthesis and pharmacological evaluation of some (E)- and (Z)-N-alkyl-alpha, beta-dimethylcinnamamides substituted on the phenyl group.
AID1129993	Anticonvulsant activity in Swiss Webster mouse assessed as survivors level at 30 mg/kg, ip pretreated 20 mins before PTZ challenge and measured 24 hrs post PTZ challenge relative to control	2014	Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7	Synthesis and anticonvulsant activity of some new pyrazolo[3,4-b]pyrazines and related heterocycles.
AID1209520	Activation of CAR in rat hepatocytes assessed as increase in CYP2B-mediated benzyloxyresorufin O-dealkylation at 100 uM after 24 hrs by spectrofluorometric analysis relative to control	2012	Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1	Species-dependent and receptor-selective action of bilobalide on the function of constitutive androstane receptor and pregnane X receptor.
AID1149322	Behavioral toxicity in po dosed albino Icem-CET (SPF Caw) mouse assessed as reduction in locomotor activity by Irwin's test	1977	Journal of medicinal chemistry, Jan, Volume: 20, Issue:1	Structure-activity relationship in cinnamamides. 2. Synthesis and pharmacological evaluation of some (E)- and (Z)-N-alkyl-alpha, beta-dimethylcinnamamides substituted on the phenyl group.
AID1145215	Central nervous depressant activity in ip dosed mouse assessed as induction of ataxia	1976	Journal of medicinal chemistry, Mar, Volume: 19, Issue:3	Synthesis and central nervous system depressant activity of some bicyclic amides.
AID1145216	Central nervous depressant activity in ip dosed mouse assessed as loss of righting reflex	1976	Journal of medicinal chemistry, Mar, Volume: 19, Issue:3	Synthesis and central nervous system depressant activity of some bicyclic amides.
AID1149329	Behavioral toxicity in po dosed albino Icem-CET (SPF Caw) mouse assessed as excitement at 25 to 100 mg/kg, po measured up to 30 mins post dose by Irwin's test	1977	Journal of medicinal chemistry, Jan, Volume: 20, Issue:1	Structure-activity relationship in cinnamamides. 2. Synthesis and pharmacological evaluation of some (E)- and (Z)-N-alkyl-alpha, beta-dimethylcinnamamides substituted on the phenyl group.
AID134479	Compound was evaluated for positional passivity after peroral administration	1981	Journal of medicinal chemistry, May, Volume: 24, Issue:5	Structure--activity relationship in cinnamamides. 3. Synthesis and anticonvulsant activity evaluation of some derivatives of (E)- and (Z)-m-(trifluoromethyl)cinnamamide.
AID136794	Compound was evaluated for loss of righting reflex after peroral administration	1981	Journal of medicinal chemistry, May, Volume: 24, Issue:5	Structure--activity relationship in cinnamamides. 3. Synthesis and anticonvulsant activity evaluation of some derivatives of (E)- and (Z)-m-(trifluoromethyl)cinnamamide.
AID1145214	Anticonvulsant activity in mouse assessed as protection against N-sulfamoylhexahydroazepine-induced convulsions	1976	Journal of medicinal chemistry, Mar, Volume: 19, Issue:3	Synthesis and central nervous system depressant activity of some bicyclic amides.
AID1149323	Behavioral toxicity in po dosed albino Icem-CET (SPF Caw) mouse assessed as positional passivity by Irwin's test	1977	Journal of medicinal chemistry, Jan, Volume: 20, Issue:1	Structure-activity relationship in cinnamamides. 2. Synthesis and pharmacological evaluation of some (E)- and (Z)-N-alkyl-alpha, beta-dimethylcinnamamides substituted on the phenyl group.
AID129823	Compound was evaluated for anticonvulsant activity in mouse after peroral administration.	1981	Journal of medicinal chemistry, May, Volume: 24, Issue:5	Structure--activity relationship in cinnamamides. 3. Synthesis and anticonvulsant activity evaluation of some derivatives of (E)- and (Z)-m-(trifluoromethyl)cinnamamide.
AID134414	Lethal dose after peroral administration	1981	Journal of medicinal chemistry, May, Volume: 24, Issue:5	Structure--activity relationship in cinnamamides. 3. Synthesis and anticonvulsant activity evaluation of some derivatives of (E)- and (Z)-m-(trifluoromethyl)cinnamamide.
AID1209515	Activation of CAR in rat hepatocytes assessed as upregulation of CYP2B1 mRNA expression at 100 uM after 24 hrs by RT-PCR analysis relative to control	2012	Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1	Species-dependent and receptor-selective action of bilobalide on the function of constitutive androstane receptor and pregnane X receptor.
AID1209541	Activation of rat CAR expressed in rat hepatocytes coexpressing CYP2B1 at 100 uM after 24 hrs by dual luciferase reporter gene assay relative to control	2012	Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1	Species-dependent and receptor-selective action of bilobalide on the function of constitutive androstane receptor and pregnane X receptor.
AID1129991	Anticonvulsant activity in Swiss Webster mouse assessed as PTZ-induced clonic seizures at 30 mg/kg, ip pretreated 20 mins before PTZ challenge and measured 1 hr post PTZ challenge relative to control	2014	Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7	Synthesis and anticonvulsant activity of some new pyrazolo[3,4-b]pyrazines and related heterocycles.
AID1132654	Neurotoxicity in ip dosed mouse by rotarod test	1978	Journal of medicinal chemistry, May, Volume: 21, Issue:5	3-Aryl- and 3-hydroxy-3-aryloctahydropyrido[2,1-c][1,4]oxazines. Synthesis, stereochemistry, and central nervous system pharmacological actions.
AID1132653	Anticonvulsant activity in ip dosed mouse assessed as protection against maximal electroshock-induced seizures	1978	Journal of medicinal chemistry, May, Volume: 21, Issue:5	3-Aryl- and 3-hydroxy-3-aryloctahydropyrido[2,1-c][1,4]oxazines. Synthesis, stereochemistry, and central nervous system pharmacological actions.
AID1145212	Acute toxicity in ip dosed Royal Hart Wistar rat	1976	Journal of medicinal chemistry, Mar, Volume: 19, Issue:3	Synthesis and central nervous system depressant activity of some bicyclic amides.
AID1132647	Stimulation of spontaneous locomotor activity in mouse at 20 mg/kg, ip measured for 30 mins relative to control	1978	Journal of medicinal chemistry, May, Volume: 21, Issue:5	3-Aryl- and 3-hydroxy-3-aryloctahydropyrido[2,1-c][1,4]oxazines. Synthesis, stereochemistry, and central nervous system pharmacological actions.
AID1149327	Anticonvulsant activity in po dosed albino Icem-CET (SPF Caw) mouse assessed as inhibition of pentylenetetrazole-induced maximal extensor seizures compound administered 30 mins prior challenge	1977	Journal of medicinal chemistry, Jan, Volume: 20, Issue:1	Structure-activity relationship in cinnamamides. 2. Synthesis and pharmacological evaluation of some (E)- and (Z)-N-alkyl-alpha, beta-dimethylcinnamamides substituted on the phenyl group.
AID135600	Locomotor activity reduction after peroral administration	1981	Journal of medicinal chemistry, May, Volume: 24, Issue:5	Structure--activity relationship in cinnamamides. 3. Synthesis and anticonvulsant activity evaluation of some derivatives of (E)- and (Z)-m-(trifluoromethyl)cinnamamide.
AID1132656	Protective index, ratio of TD50 for neurotoxicity in ip dosed mouse to ED50 for anticonvulsant activity in ip dosed mouse	1978	Journal of medicinal chemistry, May, Volume: 21, Issue:5	3-Aryl- and 3-hydroxy-3-aryloctahydropyrido[2,1-c][1,4]oxazines. Synthesis, stereochemistry, and central nervous system pharmacological actions.
AID705578	Binding affinity to NAALADase	2012	Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22	Radiofluorinated derivatives of 2-(phosphonomethyl)pentanedioic acid as inhibitors of prostate specific membrane antigen (PSMA) for the imaging of prostate cancer.
AID705577	Inhibition of NAALADase activity in human LNCaP cell membranes assessed as inhibition of [3H]NAG conversion to [3H]glutamate after 30 mins by liquid scintillation counting	2012	Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22	Radiofluorinated derivatives of 2-(phosphonomethyl)pentanedioic acid as inhibitors of prostate specific membrane antigen (PSMA) for the imaging of prostate cancer.
AID1293659	AUC (0 to t hrs) in mouse at 10 mg/kg administered via oral gavage measured after 15 mins to 4 hrs by LC/MS/MS analysis	2016	Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6	Discovery of Orally Available Prodrugs of the Glutamate Carboxypeptidase II (GCPII) Inhibitor 2-Phosphonomethylpentanedioic Acid (2-PMPA).
AID1293647	Metabolic stability in mouse plasma assessed as compound remaining at 10 uM after 1 hr by LC/MS/MS analysis	2016	Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6	Discovery of Orally Available Prodrugs of the Glutamate Carboxypeptidase II (GCPII) Inhibitor 2-Phosphonomethylpentanedioic Acid (2-PMPA).
AID773968	Displacement of [123I]-DCIT from PSMA in human LNCaP cells after 1 hr by gamma counting	2013	Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20	Preparation of asymmetric urea derivatives that target prostate-specific membrane antigen for SPECT imaging.
AID1293657	Drug level in mouse plasma treated with 30 mg/kg, ip of 4-((Bis{[(isopropoxycarbonyl)oxy]methoxy}phosphoryl)- methyl)-5-ethoxy-5-oxopentanoic acid administered via oral gavage after 30 mins by LC/MS/MS	2016	Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6	Discovery of Orally Available Prodrugs of the Glutamate Carboxypeptidase II (GCPII) Inhibitor 2-Phosphonomethylpentanedioic Acid (2-PMPA).
AID1226542	Selectivity ratio, ratio of Ki for antiTEV-tagged GCP3 extracellular portion (aa 36-740) (unknown origin) to Ki for antiTEV-tagged GCP2 extracellular portion (aa 44-750) (unknown origin)	2015	Journal of medicinal chemistry, May-28, Volume: 58, Issue:10	Design of highly potent urea-based, exosite-binding inhibitors selective for glutamate carboxypeptidase II.
AID411794	Binding affinity to PSMA in human PC3 cells assessed as cell surface binding in Tris-buffered saline buffer	2009	Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2	Multivalent scaffolds for affinity maturation of small molecule cell surface binders and their application to prostate tumor targeting.
AID1876792	Inhibition of GCPII (unknown origin)	2022	European journal of medicinal chemistry, Jan-05, Volume: 227	PSMA-targeted small-molecule docetaxel conjugate: Synthesis and preclinical evaluation.
AID1293649	Tmax in mouse at 30 mg/kg administered via oral gavage measured after 15 mins to 4 hrs by LC/MS/MS analysis	2016	Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6	Discovery of Orally Available Prodrugs of the Glutamate Carboxypeptidase II (GCPII) Inhibitor 2-Phosphonomethylpentanedioic Acid (2-PMPA).
AID1293668	Metabolic stability in mouse liver microsomes assessed as compound remaining at 10 uM after 1 hr by LC/MS/MS analysis	2016	Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6	Discovery of Orally Available Prodrugs of the Glutamate Carboxypeptidase II (GCPII) Inhibitor 2-Phosphonomethylpentanedioic Acid (2-PMPA).
AID71198	Compound was tested for inhibition of the Folate hydrolase	1996	Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2	Design, synthesis, and biological activity of a potent inhibitor of the neuropeptidase N-acetylated alpha-linked acidic dipeptidase.
AID1293658	Cmax in mouse at 10 mg/kg administered via oral gavage measured after 15 mins to 4 hrs by LC/MS/MS analysis	2016	Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6	Discovery of Orally Available Prodrugs of the Glutamate Carboxypeptidase II (GCPII) Inhibitor 2-Phosphonomethylpentanedioic Acid (2-PMPA).
AID187660	In vitro effect KCL-Evoked Giutamate at 10.0 nM	1996	Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2	Design, synthesis, and biological activity of a potent inhibitor of the neuropeptidase N-acetylated alpha-linked acidic dipeptidase.
AID246302	Neuroprotective effect against ischemic injury with median effective concentration in in rat	2005	Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7	Enantiospecificity of glutamate carboxypeptidase II inhibition.
AID1293667	Cmax in mouse at 30 mg/kg administered via oral gavage measured after 15 mins to 4 hrs by LC/MS/MS analysis	2016	Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6	Discovery of Orally Available Prodrugs of the Glutamate Carboxypeptidase II (GCPII) Inhibitor 2-Phosphonomethylpentanedioic Acid (2-PMPA).
AID1293655	Drug level in mouse plasma treated with 30 mg/kg, ip of 4-((Bis((pivaloyloxy)methoxy)phosphoryl)methyl)-5-me- thoxy-5-oxopentanoic acid administered via oral gavage after 30 mins by LC/MS/MS	2016	Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6	Discovery of Orally Available Prodrugs of the Glutamate Carboxypeptidase II (GCPII) Inhibitor 2-Phosphonomethylpentanedioic Acid (2-PMPA).
AID74532	In vitro inhibitory activity against glutamate carboxypeptidase II (GCP II) using N-acetyl-L-aspartyl-[3H]L-glutamate as a substrate	2003	Journal of medicinal chemistry, May-08, Volume: 46, Issue:10	Synthesis and biological evaluation of thiol-based inhibitors of glutamate carboxypeptidase II: discovery of an orally active GCP II inhibitor.
AID74531	Inhibition of Glutamate carboxypeptidase II	2003	Bioorganic & medicinal chemistry letters, Jul-07, Volume: 13, Issue:13	Synthesis and biological evaluation of hydroxamate-Based inhibitors of glutamate carboxypeptidase II.
AID315181	Inhibition of human recombinant NAALADase	2008	Bioorganic & medicinal chemistry, Feb-15, Volume: 16, Issue:4	Design and synthesis of a siderophore conjugate as a potent PSMA inhibitor and potential diagnostic agent for prostate cancer.
AID1293646	Metabolic stability in human liver microsomes assessed as compound remaining at 10 uM after 1 hr by LC/MS/MS analysis	2016	Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6	Discovery of Orally Available Prodrugs of the Glutamate Carboxypeptidase II (GCPII) Inhibitor 2-Phosphonomethylpentanedioic Acid (2-PMPA).
AID242379	In vitro inhibition of N-acetyl-L-aspartyl-[3H]L-glutamate binding to Glutamate carboxypeptidase II	2005	Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7	Enantiospecificity of glutamate carboxypeptidase II inhibition.
AID1846365	Inhibition of PSMA derived from human LNCaP cell lysate assessed as inhibition of NAAG hydrolysis incubated for 2 hrs in presence of NAAG by Amplex Red assay
AID1293650	AUC (0 to t hrs) in mouse at 30 mg/kg administered via oral gavage measured after 15 mins to 4 hrs by LC/MS/MS analysis	2016	Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6	Discovery of Orally Available Prodrugs of the Glutamate Carboxypeptidase II (GCPII) Inhibitor 2-Phosphonomethylpentanedioic Acid (2-PMPA).
AID179852	In vitro effect of compound on Basal Glutamate Efflux at 1.0 nM	1996	Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2	Design, synthesis, and biological activity of a potent inhibitor of the neuropeptidase N-acetylated alpha-linked acidic dipeptidase.
AID1293648	Metabolic stability in human plasma assessed as compound remaining at 10 uM after 1 hr by LC/MS/MS analysis	2016	Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6	Discovery of Orally Available Prodrugs of the Glutamate Carboxypeptidase II (GCPII) Inhibitor 2-Phosphonomethylpentanedioic Acid (2-PMPA).
AID1293666	Drug level in mouse plasma treated with 30 mg/kg, ip of 4-((Bis((pivaloyloxy)methoxy)phosphoryl)methyl)-5-oxo-5-((pivaloyloxy)methoxy)pentanoic acid administered via oral gavage after 30 mins by LC/MS/MS analysis	2016	Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6	Discovery of Orally Available Prodrugs of the Glutamate Carboxypeptidase II (GCPII) Inhibitor 2-Phosphonomethylpentanedioic Acid (2-PMPA).
AID143897	Inhibitory concentration against rat brain NAALADase (Folate hydrolase)	2001	Journal of medicinal chemistry, Nov-22, Volume: 44, Issue:24	Design and pharmacological activity of phosphinic acid based NAALADase inhibitors.
AID187659	In vitro effect KCL-Evoked Giutamate at 0.1 nM	1996	Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2	Design, synthesis, and biological activity of a potent inhibitor of the neuropeptidase N-acetylated alpha-linked acidic dipeptidase.
AID1226541	Inhibition of antiTEV-tagged GCP3 extracellular portion (aa 36-740) (unknown origin) using folyl-di-L-glutamate as substrate by HPLC-based enzymatic assay	2015	Journal of medicinal chemistry, May-28, Volume: 58, Issue:10	Design of highly potent urea-based, exosite-binding inhibitors selective for glutamate carboxypeptidase II.
AID187772	In vitro effect KCL-Evoked Glutamate at 1.0 nM	1996	Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2	Design, synthesis, and biological activity of a potent inhibitor of the neuropeptidase N-acetylated alpha-linked acidic dipeptidase.
AID74529	Concentration required for the neuroprotective effect determined by inhibition of GCP II	2003	Bioorganic & medicinal chemistry letters, Jul-07, Volume: 13, Issue:13	Synthesis and biological evaluation of hydroxamate-Based inhibitors of glutamate carboxypeptidase II.
AID74536	Inhibitory activity against expressed rat Glutamate carboxypeptidase II, using a substrate concentration of 5 uM	2001	Journal of medicinal chemistry, Feb-01, Volume: 44, Issue:3	Design of remarkably simple, yet potent urea-based inhibitors of glutamate carboxypeptidase II (NAALADase).
AID1293660	Plasma concentration in rhesus monkey at 10 mg/kg, po measured at 0.25 to 2 hrs post dose	2016	Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6	Discovery of Orally Available Prodrugs of the Glutamate Carboxypeptidase II (GCPII) Inhibitor 2-Phosphonomethylpentanedioic Acid (2-PMPA).
AID179851	In vitro effect of compound on Basal Glutamate Efflux at 0.1 nM	1996	Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2	Design, synthesis, and biological activity of a potent inhibitor of the neuropeptidase N-acetylated alpha-linked acidic dipeptidase.
AID1210717	Inhibition of GCP-2 (unknown origin)	2012	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12	Reversible disulfide formation of the glutamate carboxypeptidase II inhibitor E2072 results in prolonged systemic exposures in vivo.
AID1293665	Drug level in mouse plasma treated with 30 mg/kg, ip of 4-((Bis(((isopropoxycarbonyl)oxy)methoxy)phosphoryl)- methyl)-5-(((isopropoxycarbonyl)oxy)methoxy)-5-oxopentanoic acid administered via oral gavage after 30 mins by LC/MS/MS analysis	2016	Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6	Discovery of Orally Available Prodrugs of the Glutamate Carboxypeptidase II (GCPII) Inhibitor 2-Phosphonomethylpentanedioic Acid (2-PMPA).
AID1226540	Inhibition of antiTEV-tagged GCP2 extracellular portion (aa 44-750) (unknown origin) using folyl-di-L-glutamate as substrate by HPLC-based enzymatic assay	2015	Journal of medicinal chemistry, May-28, Volume: 58, Issue:10	Design of highly potent urea-based, exosite-binding inhibitors selective for glutamate carboxypeptidase II.
AID411795	Binding affinity to PSMA in human LNCaP cells assessed as cell surface binding in Tris-buffered saline buffer	2009	Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2	Multivalent scaffolds for affinity maturation of small molecule cell surface binders and their application to prostate tumor targeting.
AID1290367	Displacement of [125I]23 from PSMA in human LNCAP cells	2016	Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6	Preparation and Evaluation of Radiolabeled Antibody Recruiting Small Molecules That Target Prostate-Specific Membrane Antigen for Combined Radiotherapy and Immunotherapy.
AID1293656	Drug level in mouse plasma treated with 30 mg/kg, ip of 4-({Bis[(pivaloyloxy)methoxy]phosphoryl}methyl)-5-ethoxy- 5-oxopentanoic acid administered via oral gavage after 30 mins by LC/MS/MS	2016	Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6	Discovery of Orally Available Prodrugs of the Glutamate Carboxypeptidase II (GCPII) Inhibitor 2-Phosphonomethylpentanedioic Acid (2-PMPA).
AID74530	Inhibition of N-acetyl-L-aspartyl-[3H]L-glutamate binding to glutamate carboxypeptidase II (GCP II)	2003	Journal of medicinal chemistry, May-08, Volume: 46, Issue:10	Synthesis and biological evaluation of thiol-based inhibitors of glutamate carboxypeptidase II: discovery of an orally active GCP II inhibitor.
AID179853	In vitro effect of compound on Basal Glutamate Efflux at 10.0 nM	1996	Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2	Design, synthesis, and biological activity of a potent inhibitor of the neuropeptidase N-acetylated alpha-linked acidic dipeptidase.
AID74534	In vitro inhibitory activity against human Glutamate carboxypeptidase II by using fluorescent assay	2004	Journal of medicinal chemistry, Mar-25, Volume: 47, Issue:7	Synthesis of urea-based inhibitors as active site probes of glutamate carboxypeptidase II: efficacy as analgesic agents.
AID74533	Inhibitory concentration required against Glutamate carboxypeptidase II	2003	Bioorganic & medicinal chemistry letters, Jul-07, Volume: 13, Issue:13	Synthesis and biological evaluation of hydroxamate-Based inhibitors of glutamate carboxypeptidase II.
AID1508630	Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay	2021	Cell reports, 04-27, Volume: 35, Issue:4	A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347154	Primary screen GU AMC qHTS for Zika virus inhibitors	2020	Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49	Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1797657	Microplate GCPII Radioactivity-Based Assay from Article 10.1021/jm051019l: \\Structural optimization of thiol-based inhibitors of glutamate carboxypeptidase II by modification of the P1' side chain.\\	2006	Journal of medicinal chemistry, May-18, Volume: 49, Issue:10	Structural optimization of thiol-based inhibitors of glutamate carboxypeptidase II by modification of the P1' side chain.
AID1797656	Microplate GCPII Radioactivity-Based Assay from Article 10.1021/jm049258g: \\Enantiospecificity of glutamate carboxypeptidase II inhibition.\\	2005	Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7	Enantiospecificity of glutamate carboxypeptidase II inhibition.
AID1797641	Determination of Inhibition Concentration Values (IC50) from Article 10.1021/jm070133w: \\Structural insight into the pharmacophore pocket of human glutamate carboxypeptidase II.\\	2007	Journal of medicinal chemistry, Jul-12, Volume: 50, Issue:14	Structural insight into the pharmacophore pocket of human glutamate carboxypeptidase II.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	4 (4.40)	18.7374
1990's	4 (4.40)	18.2507
2000's	47 (51.65)	29.6817
2010's	31 (34.07)	24.3611
2020's	5 (5.49)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Publication Type	This drug (%)	All Drugs (%)
Trials	0 (0.00%)	5.53%
Trials	0 (0.00%)	5.53%
Reviews	0 (0.00%)	6.00%
Reviews	3 (3.53%)	6.00%
Case Studies	0 (0.00%)	4.05%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Observational	0 (0.00%)	0.25%
Other	6 (100.00%)	84.16%
Other	82 (96.47%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Classes	Roles
pk 11195 PK-11195 : A monocarboxylic acid amide obtained by formal condensation of the carboxy group of 1-(2-chlorophenyl)isoquinoline-3-carboxylic acid with the amino group of sec-butylmethylamine	2.07	1	aromatic amide; isoquinolines; monocarboxylic acid amide; monochlorobenzenes	antineoplastic agent
phenytoin [no description available]	2.36	2	imidazolidine-2,4-dione	anticonvulsant; drug allergen; sodium channel blocker; teratogenic agent
glutethimide Glutethimide: A hypnotic and sedative. Its use has been largely superseded by other drugs.	1.95	1	piperidines
ketoconazole 1-acetyl-4-(4-{[2-(2,4-dichlorophenyl)-2-(1H-imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy}phenyl)piperazine : A dioxolane that is 1,3-dioxolane which is substituted at positions 2, 2, and 4 by imidazol-1-ylmethyl, 2,4-dichlorophenyl, and [para-(4-acetylpiperazin-1-yl)phenoxy]methyl groups, respectively.	2.07	1	dichlorobenzene; dioxolane; ether; imidazoles; N-acylpiperazine; N-arylpiperazine
1,4-bis(2-(3,5-dichloropyridyloxy))benzene 1,4-bis(2-(3,5-dichloropyridyloxy))benzene: potent phenobarbital-like inducer of microsomal monooxygenase activity; structure given in first source	2.07	1
chlorpromazine hydrochloride [no description available]	1.95	1	hydrochloride; phenothiazines	anticoronaviral agent; phenothiazine antipsychotic drug
pregnenolone carbonitrile Pregnenolone Carbonitrile: A catatoxic steroid and microsomal enzyme inducer having significant effects on the induction of cytochrome P450. It has also demonstrated the potential for protective capability against acetaminophen-induced liver damage.	2.07	1	aliphatic nitrile
bilobalide [no description available]	2.07	1	sesquiterpene lactone
6-(4-chlorophenyl)imidazo(2,1-b)(1,3)thiazole-5-carbaldehyde o-(3,4-dichlorobenzyl)oxime 6-(4-chlorophenyl)imidazo(2,1-b)(1,3)thiazole-5-carbaldehyde O-(3,4-dichlorobenzyl)oxime: a constitutive androstane receptor agonist; structure in first source	2.07	1
rifampin Rifampin: A semisynthetic antibiotic produced from Streptomyces mediterranei. It has a broad antibacterial spectrum, including activity against several forms of Mycobacterium. In susceptible organisms it inhibits DNA-dependent RNA polymerase activity by forming a stable complex with the enzyme. It thus suppresses the initiation of RNA synthesis. Rifampin is bactericidal, and acts on both intracellular and extracellular organisms. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p1160)	2.07	1	cyclic ketal; hydrazone; N-iminopiperazine; N-methylpiperazine; rifamycins; semisynthetic derivative; zwitterion	angiogenesis inhibitor; antiamoebic agent; antineoplastic agent; antitubercular agent; DNA synthesis inhibitor; EC 2.7.7.6 (RNA polymerase) inhibitor; Escherichia coli metabolite; geroprotector; leprostatic drug; neuroprotective agent; pregnane X receptor agonist; protein synthesis inhibitor
formaldehyde paraform: polymerized formaldehyde; RN given refers to parent cpd; used in root canal therapy	2.73	3	aldehyde; one-carbon compound	allergen; carcinogenic agent; disinfectant; EC 3.5.1.4 (amidase) inhibitor; environmental contaminant; Escherichia coli metabolite; mouse metabolite; Saccharomyces cerevisiae metabolite
glutaric acid glutaric acid: RN given refers to parent cpd. glutaric acid : An alpha,omega-dicarboxylic acid that is a linear five-carbon dicarboxylic acid.	2.25	1	alpha,omega-dicarboxylic acid; dicarboxylic fatty acid	Daphnia magna metabolite; human metabolite
glycine [no description available]	2.41	2	alpha-amino acid; amino acid zwitterion; proteinogenic amino acid; serine family amino acid	EC 2.1.2.1 (glycine hydroxymethyltransferase) inhibitor; fundamental metabolite; hepatoprotective agent; micronutrient; neurotransmitter; NMDA receptor agonist; nutraceutical
succinic acid Succinic Acid: A water-soluble, colorless crystal with an acid taste that is used as a chemical intermediate, in medicine, the manufacture of lacquers, and to make perfume esters. It is also used in foods as a sequestrant, buffer, and a neutralizing agent. (Hawley's Condensed Chemical Dictionary, 12th ed, p1099; McGraw-Hill Dictionary of Scientific and Technical Terms, 4th ed, p1851). succinic acid : An alpha,omega-dicarboxylic acid resulting from the formal oxidation of each of the terminal methyl groups of butane to the corresponding carboxy group. It is an intermediate metabolite in the citric acid cycle.	2.25	1	alpha,omega-dicarboxylic acid; C4-dicarboxylic acid	anti-ulcer drug; fundamental metabolite; micronutrient; nutraceutical; radiation protective agent
urea pseudourea: clinical use; structure. isourea : A carboximidic acid that is the imidic acid tautomer of urea, H2NC(=NH)OH, and its hydrocarbyl derivatives.	3.46	7	isourea; monocarboxylic acid amide; one-carbon compound	Daphnia magna metabolite; Escherichia coli metabolite; fertilizer; flour treatment agent; human metabolite; mouse metabolite; Saccharomyces cerevisiae metabolite
2-amino-5-phosphonovalerate 2-Amino-5-phosphonovalerate: The D-enantiomer is a potent and specific antagonist of NMDA glutamate receptors (RECEPTORS, N-METHYL-D-ASPARTATE). The L form is inactive at NMDA receptors but may affect the AP4 (2-amino-4-phosphonobutyrate; APB) excitatory amino acid receptors.	2.03	1	non-proteinogenic alpha-amino acid	NMDA receptor antagonist
phenytoin [no description available]	2.03	1	imidazolidine-2,4-dione	anticonvulsant; drug allergen; sodium channel blocker; teratogenic agent
carbamazepine Carbamazepine: A dibenzazepine that acts as a sodium channel blocker. It is used as an anticonvulsant for the treatment of grand mal and psychomotor or focal SEIZURES. It may also be used in the management of BIPOLAR DISORDER, and has analgesic properties.. carbamazepine : A dibenzoazepine that is 5H-dibenzo[b,f]azepine carrying a carbamoyl substituent at the azepine nitrogen, used as an anticonvulsant.	2.03	1	dibenzoazepine; ureas	analgesic; anticonvulsant; antimanic drug; drug allergen; EC 3.5.1.98 (histone deacetylase) inhibitor; environmental contaminant; glutamate transporter activator; mitogen; non-narcotic analgesic; sodium channel blocker; xenobiotic
cycloleucine Cycloleucine: An amino acid formed by cyclization of leucine. It has cytostatic, immunosuppressive and antineoplastic activities.. 1-aminocyclopentanecarboxylic acid : A non-proteinogenic alpha-amino acid that is cyclopentane substituted at position 1 by amino and carboxy groups.	2.01	1	non-proteinogenic alpha-amino acid	EC 2.5.1.6 (methionine adenosyltransferase) inhibitor
valproic acid Valproic Acid: A fatty acid with anticonvulsant and anti-manic properties that is used in the treatment of EPILEPSY and BIPOLAR DISORDER. The mechanisms of its therapeutic actions are not well understood. It may act by increasing GAMMA-AMINOBUTYRIC ACID levels in the brain or by altering the properties of VOLTAGE-GATED SODIUM CHANNELS.. valproic acid : A branched-chain saturated fatty acid that comprises of a propyl substituent on a pentanoic acid stem.	2.03	1	branched-chain fatty acid; branched-chain saturated fatty acid	anticonvulsant; antimanic drug; EC 3.5.1.98 (histone deacetylase) inhibitor; GABA agent; neuroprotective agent; psychotropic drug; teratogenic agent
1-methyl-3-isobutylxanthine 1-Methyl-3-isobutylxanthine: A potent cyclic nucleotide phosphodiesterase inhibitor; due to this action, the compound increases cyclic AMP and cyclic GMP in tissue and thereby activates CYCLIC NUCLEOTIDE-REGULATED PROTEIN KINASES. 3-isobutyl-1-methylxanthine : An oxopurine that is xanthine which is substituted at positions 1 and 3 by methyl and isobutyl groups, respectively.	2.03	1	3-isobutyl-1-methylxanthine
ketamine Ketamine: A cyclohexanone derivative used for induction of anesthesia. Its mechanism of action is not well understood, but ketamine can block NMDA receptors (RECEPTORS, N-METHYL-D-ASPARTATE) and may interact with sigma receptors.. ketamine : A member of the class of cyclohexanones in which one of the hydrogens at position 2 is substituted by a 2-chlorophenyl group, while the other is substituted by a methylamino group.	2.1	1	cyclohexanones; monochlorobenzenes; secondary amino compound	analgesic; environmental contaminant; intravenous anaesthetic; neurotoxin; NMDA receptor antagonist; xenobiotic
phenobarbital Phenobarbital: A barbituric acid derivative that acts as a nonselective central nervous system depressant. It potentiates GAMMA-AMINOBUTYRIC ACID action on GABA-A RECEPTORS, and modulates chloride currents through receptor channels. It also inhibits glutamate induced depolarizations.. phenobarbital : A member of the class of barbiturates, the structure of which is that of barbituric acid substituted at C-5 by ethyl and phenyl groups.	2.03	1	barbiturates	anticonvulsant; drug allergen; excitatory amino acid antagonist; sedative
risperidone Risperidone: A selective blocker of DOPAMINE D2 RECEPTORS and SEROTONIN 5-HT2 RECEPTORS that acts as an atypical antipsychotic agent. It has been shown to improve both positive and negative symptoms in the treatment of SCHIZOPHRENIA.. risperidone : A member of the class of pyridopyrimidines that is 2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one carrying an additional 2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl group at position 2.	2.07	1	1,2-benzoxazoles; heteroarylpiperidine; organofluorine compound; pyridopyrimidine	alpha-adrenergic antagonist; dopaminergic antagonist; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; H1-receptor antagonist; psychotropic drug; second generation antipsychotic; serotonergic antagonist
dextroamphetamine Dextroamphetamine: The d-form of AMPHETAMINE. It is a central nervous system stimulant and a sympathomimetic. It has also been used in the treatment of narcolepsy and of attention deficit disorders and hyperactivity in children. Dextroamphetamine has multiple mechanisms of action including blocking uptake of adrenergics and dopamine, stimulating release of monamines, and inhibiting monoamine oxidase. It is also a drug of abuse and a psychotomimetic.. (S)-amphetamine : A 1-phenylpropan-2-amine that has S configuration.	2.47	2	1-phenylpropan-2-amine	adrenergic agent; adrenergic uptake inhibitor; dopamine uptake inhibitor; dopaminergic agent; neurotoxin; sympathomimetic agent
pilocarpine Pilocarpine: A slowly hydrolyzed muscarinic agonist with no nicotinic effects. Pilocarpine is used as a miotic and in the treatment of glaucoma.. (+)-pilocarpine : The (+)-enantiomer of pilocarpine.	2.07	1	pilocarpine	antiglaucoma drug
aspartic acid Aspartic Acid: One of the non-essential amino acids commonly occurring in the L-form. It is found in animals and plants, especially in sugar cane and sugar beets. It may be a neurotransmitter.. aspartic acid : An alpha-amino acid that consists of succinic acid bearing a single alpha-amino substituent. L-aspartic acid : The L-enantiomer of aspartic acid.	3.83	3	aspartate family amino acid; aspartic acid; L-alpha-amino acid; proteinogenic amino acid	Escherichia coli metabolite; mouse metabolite; neurotransmitter
sucrose Saccharum: A plant genus of the family POACEAE widely cultivated in the tropics for the sweet cane that is processed into sugar.	2.05	1	glycosyl glycoside	algal metabolite; Escherichia coli metabolite; human metabolite; mouse metabolite; osmolyte; Saccharomyces cerevisiae metabolite; sweetening agent
phencyclidine Phencyclidine: A hallucinogen formerly used as a veterinary anesthetic, and briefly as a general anesthetic for humans. Phencyclidine is similar to KETAMINE in structure and in many of its effects. Like ketamine, it can produce a dissociative state. It exerts its pharmacological action through inhibition of NMDA receptors (RECEPTORS, N-METHYL-D-ASPARTATE). As a drug of abuse, it is known as PCP and Angel Dust.. phencyclidine : A member of the class of piperidines that is piperidine in which the nitrogen is substituted with a 1-phenylcyclohexyl group. Formerly used as an anaesthetic agent, it exhibits both hallucinogenic and neurotoxic effects.	2.47	2	benzenes; piperidines	anaesthetic; neurotoxin; NMDA receptor antagonist; psychotropic drug
xanthenes Xanthenes: Compounds with three aromatic rings in linear arrangement with an OXYGEN in the center ring.	3.15	5	xanthene
soman Soman: An organophosphorus compound that inhibits cholinesterase. It causes seizures and has been used as a chemical warfare agent.	2.49	2	phosphonic ester
potassium cyanide [no description available]	2	1	cyanide salt; one-carbon compound; potassium salt	EC 1.15.1.1 (superoxide dismutase) inhibitor; EC 1.9.3.1 (cytochrome c oxidase) inhibitor; neurotoxin
gluconic acid gluconic acid: zinc gluconate has anti-inflammatory activity; RN given refers to (D)-isomer; all RRs refers to (D)-isomer unless otherwise noted. ketogluconic acid : A gluconic acid that contains a ketonic carbonyl group.. D-gluconic acid : A gluconic acid having D-configuration.	2.03	1	gluconic acid	chelator; Penicillium metabolite
copper gluconate Gluconates: Derivatives of gluconic acid (the structural formula HOCH2(CHOH)4COOH), including its salts and esters.	2.03	1	organic molecular entity
trinitrobenzenesulfonic acid Trinitrobenzenesulfonic Acid: A reagent that is used to neutralize peptide terminal amino groups.. 2,4,6-trinitrobenzenesulfonic acid : The arenesulfonic acid that is benzenesulfonic acid with three nitro substituents in the 2-, 4- and 6-positions.	2.15	1	arenesulfonic acid; C-nitro compound	epitope; explosive; reagent
pinacolyl methylphosphonic acid pinacolyl methylphosphonic acid: structure in first source	2.07	1
n-methylaspartate N-Methylaspartate: An amino acid that, as the D-isomer, is the defining agonist for the NMDA receptor subtype of glutamate receptors (RECEPTORS, NMDA).. N-methyl-D-aspartic acid : An aspartic acid derivative having an N-methyl substituent and D-configuration.	2.93	4	amino dicarboxylic acid; D-alpha-amino acid; D-aspartic acid derivative; secondary amino compound	neurotransmitter agent
technetium Technetium: The first artificially produced element and a radioactive fission product of URANIUM. Technetium has the atomic symbol Tc, and atomic number 43. All technetium isotopes are radioactive. Technetium 99m (m=metastable) which is the decay product of Molybdenum 99, has a half-life of about 6 hours and is used diagnostically as a radioactive imaging agent. Technetium 99 which is a decay product of technetium 99m, has a half-life of 210,000 years.	2.11	1	manganese group element atom
cysteic acid Cysteic Acid: Beta-Sulfoalanine. An amino acid with a C-terminal sulfonic acid group which has been isolated from human hair oxidized with permanganate. It occurs normally in the outer part of the sheep's fleece, where the wool is exposed to light and weather.. cysteic acid : An amino sulfonic acid that is the sulfonic acid analogue of cysteine.	2	1	alanine derivative; amino sulfonic acid; carboxyalkanesulfonic acid; cysteine derivative; non-proteinogenic alpha-amino acid	animal metabolite
glutamic acid Glutamic Acid: A non-essential amino acid naturally occurring in the L-form. Glutamic acid is the most common excitatory neurotransmitter in the CENTRAL NERVOUS SYSTEM.. glutamic acid : An alpha-amino acid that is glutaric acid bearing a single amino substituent at position 2.	5.14	14	glutamic acid; glutamine family amino acid; L-alpha-amino acid; proteinogenic amino acid	Escherichia coli metabolite; ferroptosis inducer; micronutrient; mouse metabolite; neurotransmitter; nutraceutical
quisqualic acid Quisqualic Acid: An agonist at two subsets of excitatory amino acid receptors, ionotropic receptors that directly control membrane channels and metabotropic receptors that indirectly mediate calcium mobilization from intracellular stores. The compound is obtained from the seeds and fruit of Quisqualis chinensis.	2.44	2	non-proteinogenic alpha-amino acid
cathinone cathinone: alkaloid from khat shrub, Catha edulis; RN given refers to parent cpd without isomeric designation. cathinone : The S stereoisomer of 2-aminopropiophenone.	2.15	1	2-aminopropiophenone; monoamine alkaloid	central nervous system stimulant; psychotropic drug
n-acetylaspartic acid N-acetyl-L-aspartic acid : An N-acyl-L-aspartic acid in which the acyl group is specified as acetyl.	3.83	3	N-acetyl-L-amino acid; N-acyl-L-aspartic acid	antioxidant; human metabolite; mouse metabolite; nutraceutical; rat metabolite
plasmenylserine plasmenylserine: RN given refers to (L)-isomer. O-phospho-L-serine : The L-enantiomer of O-phosphoserine.. O-phosphoserine : A serine derivative that is serine substituted at the oxygen atom by a phosphono group.	2.03	1	O-phosphoserine	EC 1.4.7.1 [glutamate synthase (ferredoxin)] inhibitor; EC 2.5.1.49 (O-acetylhomoserine aminocarboxypropyltransferase) inhibitor; EC 4.3.1.10 (serine-sulfate ammonia-lyase) inhibitor; Escherichia coli metabolite; human metabolite; mouse metabolite; Saccharomyces cerevisiae metabolite
1-amino-1,3-dicarboxycyclopentane 1-amino-1,3-dicarboxycyclopentane: RN given refers to (cis)-isomer	2.01	1
deoxyglucose Deoxyglucose: 2-Deoxy-D-arabino-hexose. An antimetabolite of glucose with antiviral activity.. deoxyglucose : A deoxyhexose comprising glucose having at least one hydroxy group replaced by hydrogen.	2	1
pyrrolidin-3-yl-methanesulfonic acid [no description available]	2	1
methotrexate [no description available]	2	1	dicarboxylic acid; monocarboxylic acid amide; pteridines	abortifacient; antimetabolite; antineoplastic agent; antirheumatic drug; dermatologic drug; DNA synthesis inhibitor; EC 1.5.1.3 (dihydrofolate reductase) inhibitor; immunosuppressive agent
docetaxel anhydrous Docetaxel: A semisynthetic analog of PACLITAXEL used in the treatment of locally advanced or metastatic BREAST NEOPLASMS and NON-SMALL CELL LUNG CANCER.. docetaxel anhydrous : A tetracyclic diterpenoid that is paclitaxel with the N-benzyloxycarbonyl group replaced by N-tert-butoxycarbonyl, and the acetoxy group at position 10 replaced by a hydroxy group.	2.41	1	secondary alpha-hydroxy ketone; tetracyclic diterpenoid	antimalarial; antineoplastic agent; photosensitizing agent
aspartylglutamate aspartylglutamate: RN given refers to all (L)-isomer	2	1	dipeptide	metabolite
alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid [no description available]	2.03	1
serine o-sulfate serine O-sulfate: RN given refers to (L)-isomer. L-serine O-sulfate : A non-proteinogenic L-alpha-amino acid that is the O-sulfo derivative of L-serine.	2.03	1	L-serine derivative; non-proteinogenic L-alpha-amino acid; O-sulfoamino acid
isospaglumic acid isospaglumic acid: mediator in the sensitivity of animals to hyperbaric oxygenation; Naaxia is the tradename; apparently can have both a neuroprotective and a neurotoxic effect. Ac-Asp-Glu : A dipeptide composed of N-acetyl-L-aspartic acid and L-glutamic acid joined by a peptide linkage.	5.69	25	dipeptide	human metabolite
sq 14,603 2-benzyl-3-mercaptopropanoic acid: structure; carboxypeptidase inhibitor	2.01	1
eglumetad eglumetad: LY-354740 is the active isomer, LY-366563 is the inactive isomer, and LY 314582 is the racemate; structure given in first source	2.06	1	L-alpha-amino acid
glutamyl-glutamic acid glutamyl-glutamic acid: RN given for (L,L)-isomer. Glu-Glu : A dipeptide composed of two L-glutamic acid units joined by a peptide linkage.	2	1	dipeptide	Mycoplasma genitalium metabolite
willardiine willardiine: isolated from seeds of Acacia willariana; structure. 3-(uracil-1-yl)-L-alanine : The 3-(uracil-1-yl) derivative of L-alanine.	2.03	1	amino acid zwitterion; L-alanine derivative; non-proteinogenic L-alpha-amino acid
cocaine Cocaine: An alkaloid ester extracted from the leaves of plants including coca. It is a local anesthetic and vasoconstrictor and is clinically used for that purpose, particularly in the eye, ear, nose, and throat. It also has powerful central nervous system effects similar to the amphetamines and is a drug of abuse. Cocaine, like amphetamines, acts by multiple mechanisms on brain catecholaminergic neurons; the mechanism of its reinforcing effects is thought to involve inhibition of dopamine uptake.. cocaine : A tropane alkaloid obtained from leaves of the South American shrub Erythroxylon coca.	3.28	6	benzoate ester; methyl ester; tertiary amino compound; tropane alkaloid	adrenergic uptake inhibitor; central nervous system stimulant; dopamine uptake inhibitor; environmental contaminant; local anaesthetic; mouse metabolite; plant metabolite; serotonin uptake inhibitor; sodium channel blocker; sympathomimetic agent; vasoconstrictor agent; xenobiotic
alpha-methyl-4-carboxyphenylglycine alpha-methyl-4-carboxyphenylglycine: glutamate receptor antagonist. (S)-alpha-methyl-4-carboxyphenylglycine : A non-proteinogenic alpha-amino acid that is alanine in which the alpha-hydrogen is replaced by a 4-carboxyphenyl group (the S-enantiomer). It is a non-selective group I/group II metabotropic glutamate receptor (mGluR) antagonist.	2.41	2	non-proteinogenic alpha-amino acid	metabotropic glutamate receptor antagonist
gamma-glutamyl hydroxamate glutamine hydroxamate : A hydroxamic acid that is L-glutamine hydroxylated at N-5.	2.01	1	amino acid zwitterion; glutamic acid derivative; hydroxamic acid
aspartyl-aspartic acid aspartyl-aspartic acid: do not confuse with cyclo(Asp-Asp). Asp-Asp : A dipeptide formed from two L-aspartic acid units.	2	1	dipeptide	Mycoplasma genitalium metabolite
leucine hydroxamate leucine hydroxamate: RN given refers to (S)-isomer	2.01	1
6-cyano-7-nitroquinoxaline-2,3-dione 6-Cyano-7-nitroquinoxaline-2,3-dione: A potent excitatory amino acid antagonist with a preference for non-NMDA iontropic receptors. It is used primarily as a research tool.	2	1	quinoxaline derivative
naloxone Naloxone: A specific opiate antagonist that has no agonist activity. It is a competitive antagonist at mu, delta, and kappa opioid receptors.. naloxone : A synthetic morphinane alkaloid that is morphinone in which the enone double bond has been reduced to a single bond, the hydrogen at position 14 has been replaced by a hydroxy group, and the methyl group attached to the nitrogen has been replaced by an allyl group. A specific opioid antagonist, it is used (commonly as its hydrochloride salt) to reverse the effects of opioids, both following their use of opioids during surgery and in cases of known or suspected opioid overdose.	2.02	1	morphinane alkaloid; organic heteropentacyclic compound; tertiary alcohol	antidote to opioid poisoning; central nervous system depressant; mu-opioid receptor antagonist
morphine Meconium: The thick green-to-black mucilaginous material found in the intestines of a full-term fetus. It consists of secretions of the INTESTINAL GLANDS; BILE PIGMENTS; FATTY ACIDS; AMNIOTIC FLUID; and intrauterine debris. It constitutes the first stools passed by a newborn.	2.02	1	morphinane alkaloid; organic heteropentacyclic compound; tertiary amino compound	anaesthetic; drug allergen; environmental contaminant; geroprotector; mu-opioid receptor agonist; opioid analgesic; plant metabolite; vasodilator agent; xenobiotic
dizocilpine maleate Dizocilpine Maleate: A potent noncompetitive antagonist of the NMDA receptor (RECEPTORS, N-METHYL-D-ASPARTATE) used mainly as a research tool. The drug has been considered for the wide variety of neurodegenerative conditions or disorders in which NMDA receptors may play an important role. Its use has been primarily limited to animal and tissue experiments because of its psychotropic effects.. dizocilpine maleate : A maleate salt obtained by reaction of dizocilpine with one equivalent of maleic acid.	2.7	3	maleate salt; tetracyclic antidepressant	anaesthetic; anticonvulsant; neuroprotective agent; nicotinic antagonist; NMDA receptor antagonist
ly 379268 LY 379268: group II metabotropic glutamate receptor agonist; structure in first source. LY 379268 : An organic heterobicyclic compound that is (1R,5S)-2-oxabicyclo[3.1.0]hexane carrying amino, carboxy, and carboxy groups at positions 4R, 4R and 6R, respectively. It is a potent agonist of group II metabotropic glutamate receptors mGluR2 and mGluR3 (EC50 = 2.69 nM and 4.48 nM, respectively) that exhibits antipsychotic-like action in animal models of schizophrenia.	2.44	2	amino dicarboxylic acid; bridged compound; organic heterobicyclic compound	antipsychotic agent; anxiolytic drug; metabotropic glutamate receptor agonist; neuroprotective agent
gpi 5693 2-(3-mercaptopropyl)pentanedioic acid: inhibits glutamate carboxypeptidase II; structure in first source	4.52	7
ly 341495 LY 341495: structure in first source	3.15	5
veratridine Veratridine: A benzoate-cevane found in VERATRUM and Schoenocaulon. It activates SODIUM CHANNELS to stay open longer than normal.	2	1
zj43 ZJ43: N-acetylaspartylglutamate (NAAG) peptidase inhibitor; structure in first source	3.46	7
dynorphins Dynorphins: A class of opioid peptides including dynorphin A, dynorphin B, and smaller fragments of these peptides. Dynorphins prefer kappa-opioid receptors (RECEPTORS, OPIOID, KAPPA) and have been shown to play a role as central nervous system transmitters.	2.02	1
picrotoxin Picrotoxin: A noncompetitive antagonist at GABA-A receptors and thus a convulsant. Picrotoxin blocks the GAMMA-AMINOBUTYRIC ACID-activated chloride ionophore. Although it is most often used as a research tool, it has been used as a CNS stimulant and an antidote in poisoning by CNS depressants, especially the barbiturates.. picrotoxin : A mixture consisting of equimolar amounts of picrotoxinin and picrotin found in the climbing plant Anamirta cocculus.	2.03	1
transforming growth factor beta Transforming Growth Factor beta: A factor synthesized in a wide variety of tissues. It acts synergistically with TGF-alpha in inducing phenotypic transformation and can also act as a negative autocrine growth factor. TGF-beta has a potential role in embryonal development, cellular differentiation, hormone secretion, and immune function. TGF-beta is found mostly as homodimer forms of separate gene products TGF-beta1, TGF-beta2 or TGF-beta3. Heterodimers composed of TGF-beta1 and 2 (TGF-beta1.2) or of TGF-beta2 and 3 (TGF-beta2.3) have been isolated. The TGF-beta proteins are synthesized as precursor proteins.	2.05	1
guanosine diphosphate Guanosine Diphosphate: A guanine nucleotide containing two phosphate groups esterified to the sugar moiety.	2.03	1	guanosine 5'-phosphate; purine ribonucleoside 5'-diphosphate	Escherichia coli metabolite; mouse metabolite; uncoupling protein inhibitor
folic acid folcysteine: used to promote fertility in chickens. vitamin B9 : Any B-vitamin that exhibits biological activity against vitamin B9 deficiency. Vitamin B9 refers to the many forms of folic acid and its derivatives, including tetrahydrofolic acid (the active form), methyltetrahydrofolate (the primary form found in blood), methenyltetrahydrofolate, folinic acid amongst others. They are present in abundance in green leafy vegetables, citrus fruits, and animal products. Lack of vitamin B9 leads to anemia, a condition in which the body cannot produce sufficient number of red blood cells. Symptoms of vitamin B9 deficiency include fatigue, muscle weakness, and pale skin.	2.05	1	folic acids; N-acyl-amino acid	human metabolite; mouse metabolite; nutrient
guanosine 5'-o-(2-thiodiphosphate) [no description available]	2.03	1	nucleoside diphosphate analogue

Condition	Relationship Strength	Studies
Action Tremor [description not available]	1.95	1
Tremor Cyclical movement of a body part that can represent either a physiologic process or a manifestation of disease. Intention or action tremor, a common manifestation of CEREBELLAR DISEASES, is aggravated by movement. In contrast, resting tremor is maximal when there is no attempt at voluntary movement, and occurs as a relatively frequent manifestation of PARKINSON DISEASE.	1.95	1
Absence Seizure [description not available]	2.73	3
Seizures Clinical or subclinical disturbances of cortical function due to a sudden, abnormal, excessive, and disorganized discharge of brain cells. Clinical manifestations include abnormal motor, sensory and psychic phenomena. Recurrent seizures are usually referred to as EPILEPSY or seizure disorder.	2.73	3
Arterial Obstructive Diseases [description not available]	2	1
Peripheral Nerve Diseases [description not available]	2.93	4
Arterial Occlusive Diseases Pathological processes which result in the partial or complete obstruction of ARTERIES. They are characterized by greatly reduced or absence of blood flow through these vessels. They are also known as arterial insufficiency.	2	1
Peripheral Nervous System Diseases Diseases of the peripheral nerves external to the brain and spinal cord, which includes diseases of the nerve roots, ganglia, plexi, autonomic nerves, sensory nerves, and motor nerves.	2.93	4
Constriction, Pathological [description not available]	2.71	3
Allodynia [description not available]	2.41	2
Ache [description not available]	3.54	8
Constriction, Pathologic The condition of an anatomical structure's being constricted beyond normal dimensions.	2.71	3
Pain An unpleasant sensation induced by noxious stimuli which are detected by NERVE ENDINGS of NOCICEPTIVE NEURONS.	3.54	8
Cerebral Ischemia [description not available]	2.93	4
Brain Ischemia Localized reduction of blood flow to brain tissue due to arterial obstruction or systemic hypoperfusion. This frequently occurs in conjunction with brain hypoxia (HYPOXIA, BRAIN). Prolonged ischemia is associated with BRAIN INFARCTION.	2.93	4
Cerebral Infarction, Middle Cerebral Artery [description not available]	2.41	2
Infarction, Middle Cerebral Artery NECROSIS occurring in the MIDDLE CEREBRAL ARTERY distribution system which brings blood to the entire lateral aspects of each CEREBRAL HEMISPHERE. Clinical signs include impaired cognition; APHASIA; AGRAPHIA; weak and numbness in the face and arms, contralaterally or bilaterally depending on the infarction.	2.41	2
Chronic Illness [description not available]	2.43	2
Chronic Disease Diseases which have one or more of the following characteristics: they are permanent, leave residual disability, are caused by nonreversible pathological alteration, require special training of the patient for rehabilitation, or may be expected to require a long period of supervision, observation, or care (Dictionary of Health Services Management, 2d ed). For epidemiological studies chronic disease often includes HEART DISEASES; STROKE; CANCER; and diabetes (DIABETES MELLITUS, TYPE 2).	2.43	2
Cancer of Prostate [description not available]	3.44	7
Prostatic Neoplasms Tumors or cancer of the PROSTATE.	3.44	7
Congenital Zika Syndrome [description not available]	2.25	1
Disease Models, Animal Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.	4.83	12
Zika Virus Infection A viral disease transmitted by the bite of AEDES mosquitoes infected with ZIKA VIRUS. Its mild DENGUE-like symptoms include fever, rash, headaches and ARTHRALGIA. The viral infection during pregnancy, in rare cases, is associated with congenital brain and ocular abnormalities, called Congenital Zika Syndrome, including MICROCEPHALY and may also lead to GUILLAIN-BARRE SYNDROME.	2.25	1
Experimental Neoplasms [description not available]	2.41	1
Acute Confusional Senile Dementia [description not available]	2.47	2
Alzheimer Disease A degenerative disease of the BRAIN characterized by the insidious onset of DEMENTIA. Impairment of MEMORY, judgment, attention span, and problem solving skills are followed by severe APRAXIAS and a global loss of cognitive abilities. The condition primarily occurs after age 60, and is marked pathologically by severe cortical atrophy and the triad of SENILE PLAQUES; NEUROFIBRILLARY TANGLES; and NEUROPIL THREADS. (From Adams et al., Principles of Neurology, 6th ed, pp1049-57)	2.47	2
Organophosphorus Poisoning [description not available]	2.11	1
Organophosphate Poisoning Poisoning due to exposure to ORGANOPHOSPHORUS COMPOUNDS, such as ORGANOPHOSPHATES; ORGANOTHIOPHOSPHATES; and ORGANOTHIOPHOSPHONATES.	2.11	1
Cognition Disorders Disorders characterized by disturbances in mental processes related to learning, thinking, reasoning, and judgment.	2.13	1
Allergic Encephalomyelitis [description not available]	2.8	3
MS (Multiple Sclerosis) [description not available]	2.5	2
Multiple Sclerosis An autoimmune disorder mainly affecting young adults and characterized by destruction of myelin in the central nervous system. Pathologic findings include multiple sharply demarcated areas of demyelination throughout the white matter of the central nervous system. Clinical manifestations include visual loss, extra-ocular movement disorders, paresthesias, loss of sensation, weakness, dysarthria, spasticity, ataxia, and bladder dysfunction. The usual pattern is one of recurrent attacks followed by partial recovery (see MULTIPLE SCLEROSIS, RELAPSING-REMITTING), but acute fulminating and chronic progressive forms (see MULTIPLE SCLEROSIS, CHRONIC PROGRESSIVE) also occur. (Adams et al., Principles of Neurology, 6th ed, p903)	2.5	2
Disease Exacerbation [description not available]	2.13	1
Bowel Diseases, Inflammatory [description not available]	2.15	1
Colitis Inflammation of the COLON section of the large intestine (INTESTINE, LARGE), usually with symptoms such as DIARRHEA (often with blood and mucus), ABDOMINAL PAIN, and FEVER.	2.15	1
Inflammatory Bowel Diseases Chronic, non-specific inflammation of the GASTROINTESTINAL TRACT. Etiology may be genetic or environmental. This term includes CROHN DISEASE and ULCERATIVE COLITIS.	2.15	1
Cocaine Abuse [description not available]	2.05	1
Cocaine-Related Disorders Disorders related or resulting from use of cocaine.	2.05	1
Acquired-Immune Deficiency Syndrome Dementia Complex [description not available]	2.05	1
AIDS Dementia Complex A neurologic condition associated with the ACQUIRED IMMUNODEFICIENCY SYNDROME and characterized by impaired concentration and memory, slowness of hand movements, ATAXIA, incontinence, apathy, and gait difficulties associated with HIV-1 viral infection of the central nervous system. Pathologic examination of the brain reveals white matter rarefaction, perivascular infiltrates of lymphocytes, foamy macrophages, and multinucleated giant cells. (From Adams et al., Principles of Neurology, 6th ed, pp760-1; N Engl J Med, 1995 Apr 6;332(14):934-40)	2.05	1
Dementia Praecox [description not available]	2.76	3
Schizophrenia A severe emotional disorder of psychotic depth characteristically marked by a retreat from reality with delusion formation, HALLUCINATIONS, emotional disharmony, and regressive behavior.	2.76	3
Cognitive Decline [description not available]	2.07	1
Cognitive Dysfunction Diminished or impaired mental and/or intellectual function.	2.07	1
Convulsions, Grand Mal [description not available]	2.01	1
Epilepsy, Tonic-Clonic A generalized seizure disorder characterized by recurrent major motor seizures. The initial brief tonic phase is marked by trunk flexion followed by diffuse extension of the trunk and extremities. The clonic phase features rhythmic flexor contractions of the trunk and limbs, pupillary dilation, elevations of blood pressure and pulse, urinary incontinence, and tongue biting. This is followed by a profound state of depressed consciousness (post-ictal state) which gradually improves over minutes to hours. The disorder may be cryptogenic, familial, or symptomatic (caused by an identified disease process). (From Adams et al., Principles of Neurology, 6th ed, p329)	2.01	1
Morphine Abuse [description not available]	2.42	2
Morphine Dependence Strong dependence, both physiological and emotional, upon morphine.	2.42	2
Acute Brain Injuries [description not available]	2.93	1
Anterior Circulation Transient Ischemic Attack [description not available]	3.33	2
Brain Injuries Acute and chronic (see also BRAIN INJURIES, CHRONIC) injuries to the brain, including the cerebral hemispheres, CEREBELLUM, and BRAIN STEM. Clinical manifestations depend on the nature of injury. Diffuse trauma to the brain is frequently associated with DIFFUSE AXONAL INJURY or COMA, POST-TRAUMATIC. Localized injuries may be associated with NEUROBEHAVIORAL MANIFESTATIONS; HEMIPARESIS, or other focal neurologic deficits.	2.93	1
Ischemic Attack, Transient Brief reversible episodes of focal, nonconvulsive ischemic dysfunction of the brain having a duration of less than 24 hours, and usually less than one hour, caused by transient thrombotic or embolic blood vessel occlusion or stenosis. Events may be classified by arterial distribution, temporal pattern, or etiology (e.g., embolic vs. thrombotic). (From Adams et al., Principles of Neurology, 6th ed, pp814-6)	3.33	2
Nerve Pain [description not available]	2.72	3
Neuritis A general term indicating inflammation of a peripheral or cranial nerve. Clinical manifestation may include PAIN; PARESTHESIAS; PARESIS; or HYPESTHESIA.	2.01	1
Neuralgia Intense or aching pain that occurs along the course or distribution of a peripheral or cranial nerve.	2.72	3
Asymmetric Diabetic Proximal Motor Neuropathy [description not available]	2.02	1
Diabetic Neuropathies Peripheral, autonomic, and cranial nerve disorders that are associated with DIABETES MELLITUS. These conditions usually result from diabetic microvascular injury involving small blood vessels that supply nerves (VASA NERVORUM). Relatively common conditions which may be associated with diabetic neuropathy include third nerve palsy (see OCULOMOTOR NERVE DISEASES); MONONEUROPATHY; mononeuropathy multiplex; diabetic amyotrophy; a painful POLYNEUROPATHY; autonomic neuropathy; and thoracoabdominal neuropathy. (From Adams et al., Principles of Neurology, 6th ed, p1325)	2.02	1
Ischemia A hypoperfusion of the BLOOD through an organ or tissue caused by a PATHOLOGIC CONSTRICTION or obstruction of its BLOOD VESSELS, or an absence of BLOOD CIRCULATION.	2.02	1
Arrhythmia [description not available]	2.03	1
Suffocation [description not available]	2.03	1
Arrhythmias, Cardiac Any disturbances of the normal rhythmic beating of the heart or MYOCARDIAL CONTRACTION. Cardiac arrhythmias can be classified by the abnormalities in HEART RATE, disorders of electrical impulse generation, or impulse conduction.	2.03	1
Asphyxia A pathological condition caused by lack of oxygen, manifested in impending or actual cessation of life.	2.03	1
Apoplexy [description not available]	2	1
Stroke A group of pathological conditions characterized by sudden, non-convulsive loss of neurological function due to BRAIN ISCHEMIA or INTRACRANIAL HEMORRHAGES. Stroke is classified by the type of tissue NECROSIS, such as the anatomic location, vasculature involved, etiology, age of the affected individual, and hemorrhagic vs. non-hemorrhagic nature. (From Adams et al., Principles of Neurology, 6th ed, pp777-810)	2	1
Injury, Ischemia-Reperfusion [description not available]	2.4	2
Reperfusion Injury Adverse functional, metabolic, or structural changes in tissues that result from the restoration of blood flow to the tissue (REPERFUSION) following ISCHEMIA.	2.4	2
Anterior Ischemic Optic Neuropathy [description not available]	2	1
Optic Neuropathy, Ischemic Ischemic injury to the OPTIC NERVE which usually affects the OPTIC DISK (optic neuropathy, anterior ischemic) and less frequently the retrobulbar portion of the nerve (optic neuropathy, posterior ischemic). The injury results from occlusion of arterial blood supply which may result from TEMPORAL ARTERITIS; ATHEROSCLEROSIS; COLLAGEN DISEASES; EMBOLISM; DIABETES MELLITUS; and other conditions. The disease primarily occurs in the sixth decade or later and presents with the sudden onset of painless and usually severe monocular visual loss. Anterior ischemic optic neuropathy also features optic disk edema with microhemorrhages. The optic disk appears normal in posterior ischemic optic neuropathy. (Glaser, Neuro-Ophthalmology, 2nd ed, p135)	2	1
Innate Inflammatory Response [description not available]	2	1
Acute Post-operative Pain [description not available]	2	1
Inflammation A pathological process characterized by injury or destruction of tissues caused by a variety of cytologic and chemical reactions. It is usually manifested by typical signs of pain, heat, redness, swelling, and loss of function.	2	1
Pain, Postoperative Pain during the period after surgery.	2	1
Lesion of Sciatic Nerve [description not available]	2.01	1
Anoxia-Ischemia, Brain [description not available]	2.01	1
Hypoxia-Ischemia, Brain A disorder characterized by a reduction of oxygen in the blood combined with reduced blood flow (ISCHEMIA) to the brain from a localized obstruction of a cerebral artery or from systemic hypoperfusion. Prolonged hypoxia-ischemia is associated with ISCHEMIC ATTACK, TRANSIENT; BRAIN INFARCTION; BRAIN EDEMA; COMA; and other conditions.	2.01	1

phenobarbital sodium

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phenobarbital sodium

Description

Cross-References

Synonyms (117)

Research Excerpts

Toxicity

Pharmacokinetics

Bioavailability

Dosage Studied

Drug Classes (2)

Protein Targets (10)

Potency Measurements

Inhibition Measurements

Activation Measurements

Biological Processes (29)

Molecular Functions (41)

Ceullar Components (7)

Bioassays (77)

Research

Studies (91)

Study Types

Related Drugs (77)

Related Conditions (76)