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inosine

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Description

5-chloro-2-(9H-fluoren-9-yl)-4-(4-methoxyphenoxy)pyridazin-3(2H)-one: an NPBWR1 antagonist; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID135398641
CHEMBL ID1556
CHEBI ID17596
SCHEMBL ID15804
MeSH IDM0011366
PubMed CID50904505
CHEMBL ID1972527
MeSH IDM0011366

Synonyms (182)

Synonym
inosina
inosinum
smr000058316
inosin
MLS000028518 ,
9-beta-d-ribofuranosyl-9h-purin-6-ol
9-beta-d-ribofuranosylhypoxanthine
CHEBI:17596 ,
9-(beta-d-ribofuranosyl)-9h-purin-6-ol
(2r,3s,4r,5r)-2-(hydroxymethyl)-5-(6-hydroxy-9h-purin-9-yl)tetrahydrofuran-3,4-diol
9.beta.-d-ribofuranosylhypoxanthine
inosinum [inn-latin]
nsc 20262
inosina [inn-spanish]
inosine [inn:jan]
beta-d-ribofuranoside, hypoxanthine-9
einecs 200-390-4
9-[(2r,3r,4s,5r)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-6,9-dihydro-3h-purin-6-one
cid_6021
bdbm22104
inosine (jan/inn)
D00054
inotin (tn)
inosie
9-.beta.-d-ribofuranosylhypoxanthine
hypoxanthine, 9-.beta.-d-ribofuranosyl-
hxr ,
trophicardyl
panholic-l
hypoxanthine ribonucleoside
.beta.-inosine
hypoxanthine d-riboside
oxiamin
nsc-20262
atorel
nsc20262
INO ,
hypoxanthine riboside
hypoxanthine nucleoside
ino 495
hypoxanthosine
.beta.-d-ribofuranoside, hypoxanthine-9
ribonosine
selfer
SMP1_000165
hypoxanthine-9-d-ribofuranoside
9-[(2r,3r,4s,5r)-3,4-dihydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl]-1h-purin-6-one
pantholic-l
hypoxanthine 9-beta-d-ribofuranoside
hypoxanthine, 9-beta-d-ribofuranosyl-
beta-inosine
1,9-dihydro-9-beta-d-ribofuranosyl-6h-purin-6-one
(-)-inosine
ai3-52241
inosine (8ci,9ci)
6h-purin-6-one, 1,9-dihydro-9-beta-d-ribofuranosyl-
inchi=1/c10h12n4o5/c15-1-4-6(16)7(17)10(19-4)14-3-13-5-8(14)11-2-12-9(5)18/h2-4,6-7,10,15-17h,1h2,(h,11,12,18)/t4-,6-,7-,10-/m1/s
hypoxanthine-ribose
iso-prinosine
58-63-9
C00294
inosine ,
inosine, >=99% (hplc)
2FQW
1A4M
2ADA
NCGC00095787-01
KBIO2_002560
KBIO3_003038
KBIO2_005128
KBIOSS_002569
KBIO2_007696
KBIOGR_002560
CMAP_000084
AC89F8E4-FD89-45EE-8B41-94DFC07AB42F
BMSE000098
I0037
BMSE000888
9-[(2r,3r,4s,5r)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-6,9-dihydro-1h-purin-6-one
inotin
CHEMBL1556
dtxcid0025993
tox21_111522
cas-58-63-9
dtxsid2045993 ,
BMSE000978
HMS2235I17
AKOS015995607
AKOS015969695
bdbm50366815
unii-5a614l51ct
5a614l51ct ,
S2442
gtpl4554
DB04335
9-[(2s,5s)-3,4-dihydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl]-1,9-dihydro-6h-purin-6-one
AM83935
SCHEMBL15804
NCGC00096119-02
tox21_111522_1
hypoxanthine-9-beta-d-ribofuranoside
inosine [mart.]
didanosine impurity b [who-ip]
didanosine impurity b [ep impurity]
inosine [who-ip]
inosine [usp impurity]
inosine [mi]
inosine [inn]
inosine [inci]
inosine [who-dd]
adenosine impurity g [ep impurity]
9-.beta.-d-ribofuranosyl-1,9-dihydro-6h-purin-6-one [who-ip]
inosine [jan]
9-.beta.-d-ribofuranosyl-1,9-dihydro-6h-purin-6-one
HY-N0092
CS-5845
catacol
AKOS024462561
OPERA_ID_1628
mfcd00066770
9-((2r,3r,4s,5r)-3,4-dihydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)-3h-purin-6(9h)-one
SR-01000721862-2
sr-01000721862
SR-01000721862-3
9-(3,4-dihydroxy-5-hydroxymethyl-tetrahydro-furan-2-yl)-1,9-dihydro-purin-6-one
9-beta-d-ribofuranosyl-1,9-dihydro-6h-purin-6-one (inosine)
adenosine imp. g (ep); inosine; didanosine imp. b (ph. int.); 9-beta-d-ribofuranosyl-1,9-dihydro-6h-purin-6-one; adenosine impurity g; didanosine impurity b
NCGC00096119-03
hypoxanthine-9-beta-delta-ribofuranoside
9-beta-delta-ribofuranosyl-hypoxanthine
9-beta-d-ribofuranosyl-hypoxanthine
9-beta-delta-ribofuranosylhypoxanthine
1,9-dihydro-9-b-d-ribofuranosyl-6h-purin-6-one
hypoxanthine-9 beta-delta-ribofuranoside
hypoxanthine-9-delta-ribofuranoside
hypoxanthine 9-beta-delta-ribofuranoside
1,9-dihydro-9-beta-delta-ribofuranosyl-6h-purin-6-one
9-b-d-ribofuranosyl-hypoxanthine
hypoxanthine-9 beta-d-ribofuranoside
9beta-d-ribofuranosylhypoxanthine
beta-delta-ribofuranoside hypoxanthine-9
9beta-delta-ribofuranosylhypoxanthine
9-b-d-ribofuranosylhypoxanthine
beta-d-ribofuranoside hypoxanthine-9
Q422564
atorel; hxr; hypoxanthine d-riboside
3h-inosine
inosine,(s)
9-((2r,3r,4s,5r)-3,4-dihydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)-1h-purin-6(9h)-one
AS-11754
BRD-K79612754-001-21-7
(2r,3s,4r,5r)-2-(hydroxymethyl)-5-(6-hydroxypurin-9-yl)oxolane-3,4-diol
cid 5274258
AMY30713
CCG-267127
NCGC00095787-05
EN300-310328
Z2681890654
BP-51105
SR-02000001098-1
sr-02000001098
ml250
MLS003675924
smr002356549
CHEMBL1972527 ,
bdbm50425598
cym 50769
1421365-63-0
5-chloro-2-(9h-fluoren-9-yl)-4-(4-methoxyphenoxy)-3(2h)-pyridazinone
AKOS024458429
cym50769, >=98% (hplc)
NCGC00379237-02
AS-16622
cym50769
NCGC00379237-04
cym-50769
5-chloro-2-(9h-fluoren-9-yl)-4-(4-methoxyphenoxy)pyridazin-3-one
cym50769 (ml250)
HY-108624
CS-0029332
5-CHLORO-2-(9H-FLUOREN-9-YL)-4-(4-METHOXYPHENOXY)PYRIDAZIN-3(2H)-ONE
F90304

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" While 10(-5) M MTX was rescued by 10(-3) M leucovorin, rescue of the toxic effect of 10(-4) M MTX by 10(-3) M leucovorin was not observed."( The reversal of methotrexate cytotoxicity to mouse bone marrow cells by leucovorin and nucleosides.
Bull, JM; Chabner, BA; Pinedo, HM; Zaharko, DS, 1976
)
0.26
"Tubercidin, an adenosine analogue, is toxic to human neuroblastoma cell lines, to peripheral blood mononuclear cells (PBMCs), and to myeloid colony-forming cells (CFU-C) as tested by a short-term labeled precursor uptake and by a clonogenic assay."( Selective protection of tubercidin toxicity by nitrobenzyl thioinosine in normal tissues but not in human neuroblastoma cells.
Barankiewicz, J; Cohen, A; Estrov, Z; Freedman, MH; Kaplinsky, C; Pawlin, G; Yeger, H, 1986
)
0.27
" The combination was also more toxic to the mice but the inclusion of nitrobenzylthioinosinate in the therapy significantly alleviated the toxicity of the drug combination."( Effect of nitrobenzylthioinosinate on the toxicity of tubercidin and ethidium against Trypanosoma gambiense.
Ikediobi, CO; Ogbunude, PO, 1982
)
0.26
" All adverse effects were recorded and categorized by severity."( One year safety and efficacy of inosine to increase the serum urate level for patients with Parkinson's disease in Japan.
Ando, R; Iwaki, H; Miyaue, N; Nagai, M; Nishikawa, N; Nomoto, M; Tada, S; Tsujii, T; Yabe, H, 2017
)
0.46
"We did not observe any adverse events requiring termination or reduction of the study drug, although uric acid crystalluria was transiently observed in a single subject."( One year safety and efficacy of inosine to increase the serum urate level for patients with Parkinson's disease in Japan.
Ando, R; Iwaki, H; Miyaue, N; Nagai, M; Nishikawa, N; Nomoto, M; Tada, S; Tsujii, T; Yabe, H, 2017
)
0.46

Pharmacokinetics

ExcerptReferenceRelevance
" Thus a single dose of ATP-MgCl2 has a half-life of less than 40 sec as ATP."( Clearance and maintenance of blood nucleotide levels with adenosine triphosphate-magnesium chloride injection.
Baue, AE; Jellinek, M; Pyrros, D; Shapiro, MJ; Sundine, M, 1992
)
0.28
" NBMPR-P and other inhibitors of nucleoside transport may have therapeutic applications in manipulation of the pharmacokinetic behavior and toxicity of nucleoside drugs."( Modification by nitrobenzylthioinosine-5'-monophosphate of pseudoisocytidine pharmacokinetics in mice and rats through inhibition of membrane transport.
Chou, TC; Kolassa, N; Paterson, AR, 1983
)
0.27
"The pharmacokinetic parameters of peldesine (BCX-34) were investigated after single and multiple oral doses in two groups of healthy adult volunteers."( Pharmacokinetics and pharmacodynamics of peldesine (BCX-34), a purine nucleoside phosphorylase inhibitor, following single and multiple oral doses in healthy volunteers.
Kisicki, J; Omura, GA; Stoltz, RR; Viegas, TX, 2000
)
0.31
" The pharmacokinetic properties of SK14-061a in rats after oral administration were then evaluated using this LC-MS method."( Pharmacokinetic properties of a novel inosine analog, 4'-cyano-2'-deoxyinosine, after oral administration in rats.
Hashimoto, M; Imoto, S; Ishiguro, T; Kohgo, S; Mitsuya, H; Otagiri, M; Taguchi, K; Yamasaki, K, 2018
)
0.48

Compound-Compound Interactions

The chemotherapeutic action of Bleomycin, applied at a dosage which induced only a non-specific tumor inhibition on HRS-sarcoma, was potentiated by combination with inosine. Inosine in combination with ADA antagonized the noradrenaline-induced positive inotropic effect and the increase in cardiac output. The increase in lifespan (ILS) of mice treated with 5'-DFUR was augmented by the combination with guanosine or inosines.

ExcerptReferenceRelevance
"The chemotherapeutic action of Bleomycin, applied at a dosage which induced only a non-specific tumor inhibition on HRS-sarcoma, was potentiated by combination with inosine."( Potentiation of the chemotherapeutic action of bleomycin by combination with inosine on HRS-sarcoma.
Osswald, H; Youssef, M, 1975
)
0.25
" Inosine in combination with ADA antagonized the noradrenaline-induced positive inotropic effect and the increase in cardiac output."( Hemodynamic effects of inosine in combination with positive and negative inotropic drugs: studies on rats in vivo.
Seesko, RC; Zimmer, HG, 1990
)
0.28
" The increase in lifespan (ILS) of mice treated with 5'-DFUR was augmented by the combination with guanosine or inosine in a dose-dependent fashion, and the maximum ILS was about 160% with the combination, while that in the case of 5'-DFUR alone was only 48% in the P388 leukemia system."( Potentiation of the chemotherapeutic action of 5'-deoxy-5-fluorouridine in combination with guanosine and related compounds.
Iigo, M; Ishitsuka, H; Miwa, M; Nitta, K, 1987
)
0.27
"We investigated the effects of 2'-deoxyinosine (d-Ino), a modulator yielding thymidine phosphorylase activity, on cellular pharmacology of 5-fluorouracil (FUra) in various human colorectal cell lines and its antitumoral activity when combined with FUra in human xenografts."( Enhanced antitumor activity of 5-fluorouracil in combination with 2'-deoxyinosine in human colorectal cell lines and human colon tumor xenografts.
Aubert, C; Catalin, J; Ciccolini, J; Cuq, P; Evrard, A; Formento, P; Milano, G; Peillard, L; Pelegrin, A, 2000
)
0.31
"A simple, fast and inexpensive method based on dispersive solid phase extraction (DSPE) combined with LC-MS was developed for simultaneous determination of 7 nucleosides and nucleobases (i."( Determination of the nucleosides and nucleobases in Tuber samples by dispersive solid-phase extraction combined with liquid chromatography-mass spectrometry.
Li, HM; Li, YY; Liu, P; Tang, YJ; Wan, DJ, 2011
)
0.37
"Alcohol consumption induced elevated liver enzymes, steatosis and inflammation, while LGG combined with inosine treatment was more significant to ameliorate these symptoms compared with LGG alone."( Lactobacillus rhamnosus GG combined with inosine ameliorates alcohol-induced liver injury through regulation of intestinal barrier and Treg/Th1 cells.
Chen, W; Chen, Y; Ge, Y; Gong, L; Guo, Y; Lin, H; Lin, J; Lu, C; Pan, T; Sun, H; Tu, Y; Wang, X; Wei, L; Xu, L; Zhu, L; Zhu, Y, 2022
)
0.72

Bioavailability

ExcerptReferenceRelevance
" Physical stressors included thermogenic microwave radiation (2,450 MHz, mean specific absorption rate of 91 W/kg) and conventional heating with hot air or hot-water bath."( Physiologic aging of mature porcine erythrocytes: effects of various metabolites, antimetabolites, and physical stressors.
Erwin, DN; Kiel, JL, 1986
)
0.27
" Pharmacokinetic analysis of BzDAG in the rat showed it to be 48% orally bioavailable (at a dose of 5 mg/kg)."( Purine nucleoside phosphorylase inhibitors: biochemical and pharmacological studies with 9-benzyl-9-deazaguanine and related compounds.
Allan, PW; Bennett, LL; Erion, MD; Montgomery, JA; Niwas, S; Noker, PE; Rose, LM, 1993
)
0.29
"0 h, and the absolute bioavailability of the oral formulation was approximately 51%."( Pharmacokinetics and pharmacodynamics of peldesine (BCX-34), a purine nucleoside phosphorylase inhibitor, following single and multiple oral doses in healthy volunteers.
Kisicki, J; Omura, GA; Stoltz, RR; Viegas, TX, 2000
)
0.31
" The absorption rate in the most proximal segment of intestinal loop was the highest."( The nucleotide derivatives inosine and inosinic acid inhibit intestinal absorption of mizoribine in rats.
Fujioka, N; Nakanishi, T; Nakashima, M; Okada, M; Suzuki, K, 2006
)
0.33
" The aims of the present study were to investigate the cellular uptake of mizoribine in CNT1- and CNT2-expressing Madin-Darby canine kidney type II (MDCKII) cells, and to evaluate the effect of salt intake on bioavailability of mizoribine in healthy Japanese volunteers with SLC28A1 565-A/A and -G/A alleles."( Effect of salt intake on bioavailability of mizoribine in healthy Japanese males.
Fukao, M; Hashimoto, Y; Ishida, K; Matsukura, H; Miyawaki, T; Taguchi, M; Uemura, O; Unadkat, JD; Watanabe, H; Zhang, Z, 2013
)
0.39
" These results suggest that the SK14-061a has favorable pharmacokinetic properties with a high bioavailability with the potential for use in oral pharmaceutical formulations, but drug-drug interactions should also be considered."( Pharmacokinetic properties of a novel inosine analog, 4'-cyano-2'-deoxyinosine, after oral administration in rats.
Hashimoto, M; Imoto, S; Ishiguro, T; Kohgo, S; Mitsuya, H; Otagiri, M; Taguchi, K; Yamasaki, K, 2018
)
0.48
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

Inosine, dosed by blinded titration to increase serum urate concentrations to 7. Repeated intraperitoneal injections (75 mg/kg for each injection) of inosine significantly enhanced RGC survival at 14 days after ON transection.

ExcerptRelevanceReference
"The chemotherapeutic action of Bleomycin, applied at a dosage which induced only a non-specific tumor inhibition on HRS-sarcoma, was potentiated by combination with inosine."( Potentiation of the chemotherapeutic action of bleomycin by combination with inosine on HRS-sarcoma.
Osswald, H; Youssef, M, 1975
)
0.25
"The administration of inosine dosed 25 mg/kg daily during 10 1/2 months prevented the development of excentric cardiac hypertrophy on the background of experimental aortic stenosis in rats, reduced the lowering of the working capacity of the animals, and partially inhibited the full development of functional and morphological myocardial changes, detected by electrocardiographic, vectorcardiographic, microscopic, and electronmicroscopic examinations."( Prevention of chronic experimental heart insufficiency by inosine.
Belenkii, EE; Kleimenova, NN; Sokolov, IK; Suzdalnitskii, RS; Tunitskay, TA, 1975
)
0.25
" In vitro dose-response curves to gastrin I, CCK, and the octapeptide of CCK (OP) demonstrated that both CCK and OP were partial agonists on the LES muscle."( Mechanism of cholecystokinin inhibition of lower esophageal sphincter pressure.
Cohen, S; DiMarino, AJ; Fisher, RS, 1975
)
0.25
" Dose-response curves studies suggested that inosine, but not uridine, has a common receptor site with epinephrine in adipose tissue."( Effects of uridine and inosine on glucose metabolism in skeletal muscle and activated lipolysis in adipose tissue.
Hait, G; Kypson, J, 1976
)
0.26
" However, the same adenosine dosage plus inosine (3."( The potentiation of the activity of adenosine on coronary blood flow, blood pressure and heart rate by inosine in the dog.
Komarek, J; Parish, GA, 1975
)
0.25
" Five men in each ribavirin dosage group completed at least 2 months of treatment."( Clinical, virologic, and immunologic effects of combination therapy with ribavirin and isoprinosine in HIV-infected homosexual men.
Courtless, J; LeLacheur, S; Meyer, WA; Parenti, DM; Paxton, H; Schlesselman, SB; Schulof, RS; Simon, GL; Sztein, MB, 1990
)
0.28
" Increasing concentrations of the highly selective adenosine A1 receptor antagonist 1,3-dipropyl-8-cyclopentylxanthine (DPCPX, 3-100 nM) produced parallel, rightward shifts of the dose-response curve for the N6-cyclopentyladenosine (CPA)-induced decrease in PS amplitude."( Adenosinergic inhibition in hippocampus is mediated by adenosine A1 receptors very similar to those of peripheral tissues.
Alzheimer, C; Kargl, L; ten Bruggencate, G, 1991
)
0.28
" Adenosine decreased the SVR in a dose-related manner at the lower dosage amounts but caused a maximum decrease in SVR at the higher dosage amounts averaging 30% below the Ringer control values."( Vascular development in chick embryos: a possible role for adenosine.
Adair, TH; Guyton, AC; Montani, JP; Strick, DM, 1989
)
0.28
" On day 7, while the subjects were taking AZT alone and on day 14 while they were receiving AZT + INPX, blood samples were obtained over a 6-hour dosing interval for measurement of AZT by a specific AZT radioimmunoassay."( Pharmacokinetics of zidovudine and concomitant inosine-pranobex in AIDS patients.
Bitonti, F; De Simone, C; Delia, S; Falciano, M; Ferrazzi, M; Sorice, F; Tzantzoglou, S, 1988
)
0.27
" Increased OXY dosage (15 mg/kg) or allopurinol (40 mg/kg) had no greater effects."( Effects of xanthine oxidase inhibition on ischemic acute renal failure in the rat.
Gmur, DJ; Zager, RA, 1989
)
0.28
"The dose-response characteristics for the effect of ATP upon cardiac function and vascular tone have been investigated in the isolated perfused rat heart."( Vascular and contractile responses to extracellular ATP: studies in the isolated rat heart.
Hearse, DJ; Hohl, CM,
)
0.13
" However, no leveling off of the dose-response curve was observed."( 6-Methylmercaptopurine riboside resistance in human lymphocytes in the in vivo somatic cell mutation test.
Tomkins, DJ; Wong, YW, 1986
)
0.27
" Although no clinical responses were documented, a modified dosage schedule of these drugs should be pursued based on the pharmacokinetic data obtained."( Phase I trial of the combination of 6-methylmercaptopurine riboside and 5-fluorouracil.
Calabresi, P; Crabtree, GW; Cummings, FJ; Murray, C; Spremulli, EN; Weitberg, AB; Wiemann, MC, 1988
)
0.27
" Versus the control group the group treated with 1-g methisoprinol injections at the dosage of 4 g daily for 7 days after surgery showed a positive effect on post-surgical immuno-depression."( [Effect of methisoprinol on postoperative immunodepression in subjects with malignant neoplasms].
Azzarello, G; Basile, F; Card\\i, F; Catania, G; Di Stefano, A; Giovinetto, A; Messina, L, 1981
)
0.26
" Forty-eight hours after MTX dosage the level of 7-hydroxymethotrexate exceeded that of MTX by ten to one."( Methotrexate cytotoxicity: studies on its reversal by folates and nucleosides.
Lankelma, J; Leyva, A; Nederbragt, H; Pinedo, HM, 1981
)
0.26
" The dosage of the associated anti-inflammatory drugs did not need to be increased, but neither was it decreased."( [Treatment of rheumatoid arthritis with isoprinosine. Personal experience].
Bonvoisin, B; Bouvier, M; Lejeune, E; Sidot, C; Touraine, F; Touraine, JL, 1983
)
0.27
" This metabolite accounted for 50% of the administered dose in orally dosed animals and 31% in iv dosed animals."( Inosiplex: metabolism and excretion of the dimethylaminoisopropanol and p-acetamidobenzoic acid components in rhesus monkeys.
Pfadenhauer, EH; Streeter, DG,
)
0.13
" Diazepam failed to further modify the dose-response curve to adenosine obtained in the presence of dipyridamole, and uptake inhibitor."( Mechanism of potentiation by diazepam of adenosine response.
Kulkarni, SK; Mehta, AK, 1984
)
0.27
" The therapeutic effect was optimal at dosage levels of the protecting agent in excess of those required in nonleukemic mice for protection against the lethal nebularine dosages used, suggesting that the therapeutic effect was due to the joint presence in the leukemic cells of a metabolite of NBMPR-P and nebularine; NBMPR-P protection of the leukemic host against nebularine lethality was necessary for the therapeutic effect to be manifested."( Therapy of mouse leukemia L1210 with combinations of nebularine and nitrobenzylthioinosine 5'-monophosphate.
Lynch, TP; Paran, JH; Paterson, AR, 1981
)
0.26
" In spite of common gene dosage effects, unexpected and highly significant differences were noted between Down's syndrome patients without complications and those presenting with additional psychotic features."( Differences in purine metabolism in patients with Down's syndrome.
Cattaneo, F; Lejeune, J; Megarbane, A; Peeters, MA; Rethore, MO, 1993
)
0.29
"The two basic aims of this study were to add to the limited literature concerning Inosine as an ergogenic aid, and to determine the effects of Inosine supplementation over a period of 5 and 10 days, at a dosage of 10,000 mg."( Inosine supplementation has no effect on aerobic or anaerobic cycling performance.
Dalton, B; McNaughton, L; Tarr, J, 1999
)
0.3
" Serial blood samples and total urine outputs were collected during dosing and for at least 24 hours after the last dose was administered."( Pharmacokinetics and pharmacodynamics of peldesine (BCX-34), a purine nucleoside phosphorylase inhibitor, following single and multiple oral doses in healthy volunteers.
Kisicki, J; Omura, GA; Stoltz, RR; Viegas, TX, 2000
)
0.31
" Caffeine, theophylline, and paraxanthine shifted the dose-response curve for adenosine at the A1, A2A, and A2B receptors."( Comparison of the potency of adenosine as an agonist at human adenosine receptors expressed in Chinese hamster ovary cells.
Fredholm, BB; Irenius, E; Kull, B; Schulte, G, 2001
)
0.31
" Dose-response relationships for phenylisopropyladenosine (PIA) were determined for hearts adrenergically stimulated by isoproterenol."( Chronic ethanol enhances adenosine antiadrenergic actions in the isolated rat heart.
Chung, ES; Fenton , RA, 2001
)
0.31
" Repeated intraperitoneal injections (75 mg/kg for each injection) of inosine significantly enhanced RGC survival at 14 days after ON transection (500 +/- 38), whereas no significant difference in the densities was detected at 7 days (974 +/- 101), even when the dosage of inosine was doubled (1039 +/- 61)."( Neuroprotective effect of inosine on axotomized retinal ganglion cells in adult rats.
Hou, B; Jiao, XY; Ju, G; Kuang, F; Liu, HL; Wu, MM; You, SW, 2004
)
0.32
" Inosine was administered to the Inosine treatment group by intraperitoneal injection immediately after HIBD at the dosage of 100 mg/kg twice daily for 7 days."( Effects of inosine on neuronal apoptosis and the expression of cytochrome C mRNA following hypoxic-ischemic brain damage in neonatal rats.
Deng, YH; Hei, MY; Kuang, SJ; Tian, L, 2006
)
0.33
" The dosage of inosine required for protection is very high because of the rapid metabolism of inosine in vivo."( The novel inosine analogue, INO-2002, protects against diabetes development in multiple low-dose streptozotocin and non-obese diabetic mouse models of type I diabetes.
Mabley, JG; Murthy, KG; Pacher, P; Salzman, AL; Southan, GJ; Szabo, C; Williams, W, 2008
)
0.35
" The dosage of inosine required for these effects has been shown to be between 200 and 600 mg kg(-1) because of the rapid metabolism of inosine in vivo."( The novel inosine analogue INO-2002 exerts an anti-inflammatory effect in a murine model of acute lung injury.
Mabley, JG; Murthy, KG; Pacher, P; Salzman, AL; Southan, GJ; Szabo, C; Williams, W, 2009
)
0.35
"018 mL 100g-1 body weight) once a day for 6 continuous weeks; the fibrosis rats were treated with the same dosage of physiological saline with the same frequency and time span."( [Gene expression changes of regucalcin and prohibitin in cirrhotic rat liver and the related effects of compound glutathione inosine injection intervention].
Cheng, ML; Liang, YD; Liu, JY; Liu, Y; Lu, S; Wu, J, 2014
)
0.4
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (4)

RoleDescription
human metaboliteAny mammalian metabolite produced during a metabolic reaction in humans (Homo sapiens).
Saccharomyces cerevisiae metaboliteAny fungal metabolite produced during a metabolic reaction in Baker's yeast (Saccharomyces cerevisiae).
Escherichia coli metaboliteAny bacterial metabolite produced during a metabolic reaction in Escherichia coli.
mouse metaboliteAny mammalian metabolite produced during a metabolic reaction in a mouse (Mus musculus).
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (2)

ClassDescription
inosinesAny purine ribonucleoside that is a derivative of inosine.
purines D-ribonucleosideA purine ribonucleoside that is a purine derivative attached to a beta-D-ribofuranosyl residue at position 9 via a glycosidic (N-glycosyl) linkage.
[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]

Pathways (23)

PathwayProteinsCompounds
Abacavir ADME624
Abacavir metabolism423
Metabolism of proteins1058144
Surfactant metabolism1611
guanine and guanosine salvage III010
purine nucleosides salvage II (plant)419
S-adenosyl-L-methionine cycle II427
adenosine nucleotides degradation I327
superpathway of purines degradation in plants745
purine nucleotides degradation I (plants)334
Purine nucleotides and Nucleosides metabolism ( Purine nucleotides and Nucleosides metabolism )10577
Inosine + Orthophosphate = Hypoxanthine + D-Ribose 1-phosphate ( Purine nucleotides and Nucleosides metabolism )13
Purine metabolism1336
Renz2020 - GEM of Human alveolar macrophage with SARS-CoV-20490
Drug ADME6387
Ribavirin ADME916
adenine and adenosine salvage III012
salvage pathways of purine nucleosides021
salvage pathways of adenine, hypoxanthine, and their nucleosides023
salvage pathways of purine nucleosides I027
Biochemical pathways: part I0466
Purine metabolism and related disorders2353
Purine metabolism938
Urate synthesis211

Protein Targets (26)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, Ferritin light chainEquus caballus (horse)Potency0.89135.623417.292931.6228AID485281
AR proteinHomo sapiens (human)Potency18.95860.000221.22318,912.5098AID1259247; AID743054
Smad3Homo sapiens (human)Potency0.11220.00527.809829.0929AID588855
bromodomain adjacent to zinc finger domain 2BHomo sapiens (human)Potency0.70790.707936.904389.1251AID504333
IDH1Homo sapiens (human)Potency20.59620.005210.865235.4813AID686970
v-jun sarcoma virus 17 oncogene homolog (avian)Homo sapiens (human)Potency0.00240.057821.109761.2679AID1159526
nuclear factor erythroid 2-related factor 2 isoform 2Homo sapiens (human)Potency29.09290.00419.984825.9290AID504444
gemininHomo sapiens (human)Potency5.80480.004611.374133.4983AID624296
survival motor neuron protein isoform dHomo sapiens (human)Potency1.25890.125912.234435.4813AID1458
muscleblind-like protein 1 isoform 1Homo sapiens (human)Potency0.15850.00419.962528.1838AID2675
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency6.74120.01237.983543.2770AID1645841
GVesicular stomatitis virusPotency9.52210.01238.964839.8107AID1645842
Interferon betaHomo sapiens (human)Potency9.52210.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency9.52210.01238.964839.8107AID1645842
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency9.52210.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency9.52210.01238.964839.8107AID1645842
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, ADENOSINE DEAMINASEMus musculus (house mouse)Ki0.00000.00000.00000.0000AID977610
Chain A, ADENOSINE DEAMINASEMus musculus (house mouse)Ki0.00000.00000.00000.0000AID977610
AdenosylhomocysteinaseHomo sapiens (human)Ki925.00000.00000.18991.9300AID199747
Adenosine deaminase Bos taurus (cattle)Ki500.00000.00000.48937.0000AID33651
Neuropeptides B/W receptor type 1Homo sapiens (human)IC50 (µMol)0.12000.12000.22000.2700AID724071
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, Membrane lipoprotein tmpCTreponema pallidumKd0.21000.07100.18370.2700AID977611
Chain A, Membrane lipoprotein tmpCTreponema pallidumKd0.21000.07100.18370.2700AID977611
Chain A, Membrane lipoprotein tmpCTreponema pallidumKd0.21000.07100.18370.2700AID977611
glycogen synthase kinase-3 beta isoform 1Homo sapiens (human)EC50 (µMol)300.00000.212522.156283.9400AID434954
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
AdenosylhomocysteinaseHomo sapiens (human)Km2.50000.82001.66002.5000AID199751
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (73)

Processvia Protein(s)Taxonomy
inosine catabolic processPurine nucleoside phosphorylaseHomo sapiens (human)
urate biosynthetic processPurine nucleoside phosphorylaseHomo sapiens (human)
positive regulation of T cell proliferationPurine nucleoside phosphorylaseHomo sapiens (human)
positive regulation of alpha-beta T cell differentiationPurine nucleoside phosphorylaseHomo sapiens (human)
allantoin metabolic processPurine nucleoside phosphorylaseHomo sapiens (human)
nucleobase-containing compound metabolic processPurine nucleoside phosphorylaseHomo sapiens (human)
inosine catabolic processPurine nucleoside phosphorylaseHomo sapiens (human)
deoxyinosine catabolic processPurine nucleoside phosphorylaseHomo sapiens (human)
deoxyadenosine catabolic processPurine nucleoside phosphorylaseHomo sapiens (human)
purine ribonucleoside salvagePurine nucleoside phosphorylaseHomo sapiens (human)
IMP catabolic processPurine nucleoside phosphorylaseHomo sapiens (human)
nicotinamide riboside catabolic processPurine nucleoside phosphorylaseHomo sapiens (human)
immune responsePurine nucleoside phosphorylaseHomo sapiens (human)
nucleotide biosynthetic processPurine nucleoside phosphorylaseHomo sapiens (human)
response to xenobiotic stimulusPurine nucleoside phosphorylaseHomo sapiens (human)
positive regulation of interleukin-2 productionPurine nucleoside phosphorylaseHomo sapiens (human)
purine-containing compound salvagePurine nucleoside phosphorylaseHomo sapiens (human)
dAMP catabolic processPurine nucleoside phosphorylaseHomo sapiens (human)
one-carbon metabolic processAdenosylhomocysteinaseHomo sapiens (human)
S-adenosylmethionine cycleAdenosylhomocysteinaseHomo sapiens (human)
adenosine catabolic processAdenosine deaminase Bos taurus (cattle)
cell adhesionAdenosine deaminase Bos taurus (cattle)
nucleotide metabolic processAdenosine deaminase Bos taurus (cattle)
purine ribonucleoside monophosphate biosynthetic processAdenosine deaminase Bos taurus (cattle)
inosine biosynthetic processAdenosine deaminase Bos taurus (cattle)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
positive regulation of T cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
adaptive immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-independentHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of T cell anergyHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
defense responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
detection of bacteriumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-12 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-6 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protection from natural killer cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
innate immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of dendritic cell differentiationHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class IbHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
G protein-coupled receptor signaling pathwayNeuropeptides B/W receptor type 1Homo sapiens (human)
chemical synaptic transmissionNeuropeptides B/W receptor type 1Homo sapiens (human)
regulation of metabolic processNeuropeptides B/W receptor type 1Homo sapiens (human)
G protein-coupled opioid receptor signaling pathwayNeuropeptides B/W receptor type 1Homo sapiens (human)
neuropeptide signaling pathwayNeuropeptides B/W receptor type 1Homo sapiens (human)
inositol phosphate metabolic processInositol hexakisphosphate kinase 1Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
negative regulation of cold-induced thermogenesisInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (32)

Processvia Protein(s)Taxonomy
nucleoside bindingPurine nucleoside phosphorylaseHomo sapiens (human)
purine nucleobase bindingPurine nucleoside phosphorylaseHomo sapiens (human)
purine-nucleoside phosphorylase activityPurine nucleoside phosphorylaseHomo sapiens (human)
protein bindingPurine nucleoside phosphorylaseHomo sapiens (human)
phosphate ion bindingPurine nucleoside phosphorylaseHomo sapiens (human)
identical protein bindingPurine nucleoside phosphorylaseHomo sapiens (human)
guanosine phosphorylase activityPurine nucleoside phosphorylaseHomo sapiens (human)
adenosylhomocysteinase activityAdenosylhomocysteinaseHomo sapiens (human)
protein bindingAdenosylhomocysteinaseHomo sapiens (human)
adenosine deaminase activityAdenosine deaminase Bos taurus (cattle)
protein bindingAdenosine deaminase Bos taurus (cattle)
zinc ion bindingAdenosine deaminase Bos taurus (cattle)
2'-deoxyadenosine deaminase activityAdenosine deaminase Bos taurus (cattle)
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
signaling receptor bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
peptide antigen bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein-folding chaperone bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
G protein-coupled opioid receptor activityNeuropeptides B/W receptor type 1Homo sapiens (human)
protein bindingNeuropeptides B/W receptor type 1Homo sapiens (human)
neuropeptide receptor activityNeuropeptides B/W receptor type 1Homo sapiens (human)
neuropeptide bindingNeuropeptides B/W receptor type 1Homo sapiens (human)
G protein-coupled receptor activityNeuropeptides B/W receptor type 1Homo sapiens (human)
inositol-1,3,4,5,6-pentakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol heptakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
ATP bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 1-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 3-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (30)

Processvia Protein(s)Taxonomy
extracellular regionPurine nucleoside phosphorylaseHomo sapiens (human)
cytoplasmPurine nucleoside phosphorylaseHomo sapiens (human)
cytosolPurine nucleoside phosphorylaseHomo sapiens (human)
secretory granule lumenPurine nucleoside phosphorylaseHomo sapiens (human)
extracellular exosomePurine nucleoside phosphorylaseHomo sapiens (human)
ficolin-1-rich granule lumenPurine nucleoside phosphorylaseHomo sapiens (human)
cytoplasmPurine nucleoside phosphorylaseHomo sapiens (human)
nucleusAdenosylhomocysteinaseHomo sapiens (human)
endoplasmic reticulumAdenosylhomocysteinaseHomo sapiens (human)
cytosolAdenosylhomocysteinaseHomo sapiens (human)
melanosomeAdenosylhomocysteinaseHomo sapiens (human)
extracellular exosomeAdenosylhomocysteinaseHomo sapiens (human)
cytosolAdenosylhomocysteinaseHomo sapiens (human)
lysosomeAdenosine deaminase Bos taurus (cattle)
cytoplasmic vesicle lumenAdenosine deaminase Bos taurus (cattle)
anchoring junctionAdenosine deaminase Bos taurus (cattle)
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
Golgi membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
endoplasmic reticulumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
Golgi apparatusHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
cell surfaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
ER to Golgi transport vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
secretory granule membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
phagocytic vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
early endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
recycling endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular exosomeHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
lumenal side of endoplasmic reticulum membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
MHC class I protein complexHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular spaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
external side of plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membraneNeuropeptides B/W receptor type 1Homo sapiens (human)
membraneNeuropeptides B/W receptor type 1Homo sapiens (human)
synapseNeuropeptides B/W receptor type 1Homo sapiens (human)
plasma membraneNeuropeptides B/W receptor type 1Homo sapiens (human)
neuron projectionNeuropeptides B/W receptor type 1Homo sapiens (human)
fibrillar centerInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
cytosolInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleusInositol hexakisphosphate kinase 1Homo sapiens (human)
cytoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (111)

Assay IDTitleYearJournalArticle
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
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.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
AID1745845Primary qHTS for Inhibitors of ATXN expression
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.
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.
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.
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.
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.
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.
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.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
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.
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.
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.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
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.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID216185Anti-Herpes simplex virus type-1 activity in vero cells using plaque inhibition assay1999Journal of medicinal chemistry, Aug-26, Volume: 42, Issue:17
Virtual combinatorial syntheses and computational screening of new potential anti-herpes compounds.
AID1272193Prodrug activation assessed as recombinant human PNP-mediated compound cleavage at 100 uM by reverse phase HPLC analysis2016European journal of medicinal chemistry, Jan-27, Volume: 1086-Methylpurine derived sugar modified nucleosides: Synthesis and in vivo antitumor activity in D54 tumor expressing M64V-Escherichia coli purine nucleoside phosphorylase.
AID70684Inhibition of Cellular Replication of friend erythroleukemia cells1985Journal of medicinal chemistry, Oct, Volume: 28, Issue:10
Purine and 8-substituted purine arabinofuranosyl and ribofuranosyl nucleoside derivatives as potential inducers of the differentiation of the Friend erythroleukemia.
AID401477Displacement of [3H]diazepam from benzodiazepine receptor in rat cerebral cortex membrane
AID1578763Binding affinity to human PNP assessed as catalytic rate by measuring uric acid formation2019Journal of medicinal chemistry, 09-26, Volume: 62, Issue:18
Plasmodium Purine Metabolism and Its Inhibition by Nucleoside and Nucleotide Analogues.
AID1136399Activity of human erythrocyte purine nucleoside phosphorylase assessed as ribose relase at 5 umol after 30 mins by orcinol reaction relative to guanosine1978Journal of medicinal chemistry, Sep, Volume: 21, Issue:9
Stereoelectronic factors in the binding of substrate analogues and inhibitors to purine nucleoside phosphorylase isolated from human erythrocytes.
AID199751Enzyme kinetic constant for S-adenosyl-L-homocysteine hydrolase2003Bioorganic & medicinal chemistry letters, Jun-16, Volume: 13, Issue:12
Unexpected inhibition of S-adenosyl-L-homocysteine hydrolase by a guanosine nucleoside.
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.
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.
AID681959TP_TRANSPORTER: inhibition of MPP+ uptake (MPP+: 0.15 uM, Inosine: 1000 uM) in Xenopus laevis oocytes1997Molecular pharmacology, Jun, Volume: 51, Issue:6
Cloning and functional expression of a human liver organic cation transporter.
AID584550Cytotoxicity against mouse J774A1 cells2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
Testing nucleoside analogues as inhibitors of Bacillus anthracis spore germination in vitro and in macrophage cell culture.
AID409919Activity at human PNP His257Gly mutant2008Bioorganic & medicinal chemistry letters, Nov-15, Volume: 18, Issue:22
Immucillins in custom catalytic-site cavities.
AID1571173Inhibition of Crithidia fasciculata nucleoside hydrolase2018MedChemComm, Dec-01, Volume: 9, Issue:12
The transition to magic bullets - transition state analogue drug design.
AID1272198Prodrug activation assessed as recombinant Sulfolobus solfataricus MTAP-mediated compound cleavage at 100 uM by reverse phase HPLC analysis2016European journal of medicinal chemistry, Jan-27, Volume: 1086-Methylpurine derived sugar modified nucleosides: Synthesis and in vivo antitumor activity in D54 tumor expressing M64V-Escherichia coli purine nucleoside phosphorylase.
AID1272200Prodrug activation assessed as Francisella tularensis PNP-mediated compound cleavage at 100 uM by reverse phase HPLC analysis2016European journal of medicinal chemistry, Jan-27, Volume: 1086-Methylpurine derived sugar modified nucleosides: Synthesis and in vivo antitumor activity in D54 tumor expressing M64V-Escherichia coli purine nucleoside phosphorylase.
AID684325Activity of Leishmania donovani recombinant nucleoside hydrolase expressed in Escherichia coli DH5alpha coexpressing MBP2012European journal of medicinal chemistry, Oct, Volume: 56Kinetics and docking studies of two potential new inhibitors of the nucleoside hydrolase from Leishmania donovani.
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.
AID199616Enzyme catalytic rate kinetic constant for S-adenosyl-L-homocysteine hydrolase2003Bioorganic & medicinal chemistry letters, Jun-16, Volume: 13, Issue:12
Unexpected inhibition of S-adenosyl-L-homocysteine hydrolase by a guanosine nucleoside.
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.
AID662565Growth inhibition of Trichomonas vaginalis T1 at 100 uM after 24 hrs by hemocytometry2012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
S-Adenosylhomocysteine hydrolase of the protozoan parasite Trichomonas vaginalis: potent inhibitory activity of 9-(2-deoxy-2-fluoro-β,D-arabinofuranosyl)adenine.
AID1090673Inhibition of ATP sythesis in freshly lysed Spinacia oleracea (spinach) chloroplasts2007Journal of agricultural and food chemistry, May-16, Volume: 55, Issue:10
Inhibition of photophosphorylation and electron transport chain in thylakoids by lasiodiplodin, a natural product from Botryosphaeria rhodina.
AID1272195Prodrug activation assessed as recombinant Escherichia coli PNP-mediated compound cleavage at 100 uM by reverse phase HPLC analysis2016European journal of medicinal chemistry, Jan-27, Volume: 1086-Methylpurine derived sugar modified nucleosides: Synthesis and in vivo antitumor activity in D54 tumor expressing M64V-Escherichia coli purine nucleoside phosphorylase.
AID409915Activity at wild type human PNP2008Bioorganic & medicinal chemistry letters, Nov-15, Volume: 18, Issue:22
Immucillins in custom catalytic-site cavities.
AID399372Deterrent activity against Perknaster fuscus assessed as induction of sustained retractions of tube-feet by sea-star deterrent assay1998Journal of natural products, Jan, Volume: 61, Issue:1
Purine and nucleoside metabolites from the Antarctic sponge Isodictya erinacea.
AID70559Percent benzidine-positive cell differentiation in friend erythroleukemia cells1985Journal of medicinal chemistry, Oct, Volume: 28, Issue:10
Purine and 8-substituted purine arabinofuranosyl and ribofuranosyl nucleoside derivatives as potential inducers of the differentiation of the Friend erythroleukemia.
AID492558Half life in human patient at 200 to 800 mg, iv2010Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12
Evolution of poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors. From concept to clinic.
AID1452128Inhibition of ATPgammaS-BODIPY binding to Thermotoga maritima His-tagged HK853 expressed in Escherichia coli BL21(DE3)pLysS Rosetta preincubated for 30 mins prior to ATPgammaS-BODIPY addition measured after 1 hr by coomassie staining-based SDS-PAGE analys2017Journal of medicinal chemistry, 10-12, Volume: 60, Issue:19
Rational Design of Selective Adenine-Based Scaffolds for Inactivation of Bacterial Histidine Kinases.
AID199747Inhibitory activity against S-adenosyl-L-homocysteine hydrolase was determined2003Bioorganic & medicinal chemistry letters, Jun-16, Volume: 13, Issue:12
Unexpected inhibition of S-adenosyl-L-homocysteine hydrolase by a guanosine nucleoside.
AID1272197Prodrug activation assessed as recombinant Trichomonas vaginalis PNP-mediated compound cleavage at 100 uM by reverse phase HPLC analysis2016European journal of medicinal chemistry, Jan-27, Volume: 1086-Methylpurine derived sugar modified nucleosides: Synthesis and in vivo antitumor activity in D54 tumor expressing M64V-Escherichia coli purine nucleoside phosphorylase.
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.
AID1155776Half life of the compound in trifluoroacetate buffer at 50 uM at pH 1.2 by HPLC analysis2014European journal of medicinal chemistry, Jul-23, Volume: 82Microwave-assisted synthesis of C-8 aryl and heteroaryl inosines and determination of their inhibitory activities against Plasmodium falciparum purine nucleoside phosphorylase.
AID1578764Binding affinity to Plasmodium falciparum His-tagged PNP assessed as catalytic rate by measuring uric acid formation2019Journal of medicinal chemistry, 09-26, Volume: 62, Issue:18
Plasmodium Purine Metabolism and Its Inhibition by Nucleoside and Nucleotide Analogues.
AID70686Optimum concentration for differentiation of friend erythroleukemia cells1985Journal of medicinal chemistry, Oct, Volume: 28, Issue:10
Purine and 8-substituted purine arabinofuranosyl and ribofuranosyl nucleoside derivatives as potential inducers of the differentiation of the Friend erythroleukemia.
AID33651Ability to inhibit adenosine deaminase1987Journal of medicinal chemistry, Jun, Volume: 30, Issue:6
Synthesis, structure, and biological activity of certain 2-deoxy-beta-D-ribo-hexopyranosyl nucleosides and nucleotides.
AID977611Experimentally measured binding affinity data (Kd) for protein-ligand complexes derived from PDB2006The Journal of biological chemistry, Mar-24, Volume: 281, Issue:12
The PnrA (Tp0319; TmpC) lipoprotein represents a new family of bacterial purine nucleoside receptor encoded within an ATP-binding cassette (ABC)-like operon in Treponema pallidum.
AID1811Experimentally measured binding affinity data derived from PDB2006The Journal of biological chemistry, Mar-24, Volume: 281, Issue:12
The PnrA (Tp0319; TmpC) lipoprotein represents a new family of bacterial purine nucleoside receptor encoded within an ATP-binding cassette (ABC)-like operon in Treponema pallidum.
AID1811Experimentally measured binding affinity data derived from PDB1998Biochemistry, Jun-09, Volume: 37, Issue:23
Complexes of adenosine deaminase with two potent inhibitors: X-ray structures in four independent molecules at pH of maximum activity.
AID977610Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB1998Biochemistry, Jun-09, Volume: 37, Issue:23
Complexes of adenosine deaminase with two potent inhibitors: X-ray structures in four independent molecules at pH of maximum activity.
AID977610Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB1991Science (New York, N.Y.), May-31, Volume: 252, Issue:5010
Atomic structure of adenosine deaminase complexed with a transition-state analog: understanding catalysis and immunodeficiency mutations.
AID1811Experimentally measured binding affinity data derived from PDB1991Science (New York, N.Y.), May-31, Volume: 252, Issue:5010
Atomic structure of adenosine deaminase complexed with a transition-state analog: understanding catalysis and immunodeficiency mutations.
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.
AID724071Antagonist activity against human NPBWR1 expressed in HEK293 cells co-expressing Gqi3 assessed as inhibition of agonist-induced response by FLIPR assay2013Bioorganic & medicinal chemistry letters, Feb-01, Volume: 23, Issue:3
SAR analysis of novel non-peptidic NPBWR1 (GPR7) antagonists.
AID723839Inhibition of CYP2C19 (unknown origin) at 30 uM2013Bioorganic & medicinal chemistry letters, Feb-01, Volume: 23, Issue:3
SAR analysis of novel non-peptidic NPBWR1 (GPR7) antagonists.
AID723842Half life in PBS buffer at pH 7.42013Bioorganic & medicinal chemistry letters, Feb-01, Volume: 23, Issue:3
SAR analysis of novel non-peptidic NPBWR1 (GPR7) antagonists.
AID723844Toxicity against human U2OS cells at 20 uM2013Bioorganic & medicinal chemistry letters, Feb-01, Volume: 23, Issue:3
SAR analysis of novel non-peptidic NPBWR1 (GPR7) antagonists.
AID723841Inhibition of CYP1A2 (unknown origin) at 30 uM2013Bioorganic & medicinal chemistry letters, Feb-01, Volume: 23, Issue:3
SAR analysis of novel non-peptidic NPBWR1 (GPR7) antagonists.
AID723840Inhibition of 5HT2B (unknown origin) at 30 uM2013Bioorganic & medicinal chemistry letters, Feb-01, Volume: 23, Issue:3
SAR analysis of novel non-peptidic NPBWR1 (GPR7) antagonists.
AID723843Solubility in PBS buffer at pH 7.42013Bioorganic & medicinal chemistry letters, Feb-01, Volume: 23, Issue:3
SAR analysis of novel non-peptidic NPBWR1 (GPR7) antagonists.
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.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
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.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).2014Journal of biomolecular screening, Jul, Volume: 19, Issue:6
A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (3,507)

TimeframeStudies, This Drug (%)All Drugs %
pre-19901661 (47.36)18.7374
1990's530 (15.11)18.2507
2000's520 (14.83)29.6817
2010's530 (15.11)24.3611
2020's266 (7.58)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 48.91

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 strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index48.91 (24.57)
Research Supply Index1.95 (2.92)
Research Growth Index4.51 (4.65)
Search Engine Demand Index109.49 (26.88)
Search Engine Supply Index3.06 (0.95)

This Compound (48.91)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials120 (3.22%)5.53%
Trials0 (0.00%)5.53%
Reviews169 (4.54%)6.00%
Reviews0 (0.00%)6.00%
Case Studies51 (1.37%)4.05%
Case Studies0 (0.00%)4.05%
Observational1 (0.03%)0.25%
Observational0 (0.00%)0.25%
Other3,381 (90.84%)84.16%
Other6 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]