Page last updated: 2024-08-02 17:09:21

arterolane

Description

arterolane: a trioxolane with antimalarial activity; structure in first source [MeSH]

Cross-References

ID SourceID
PubMed CID10475633
CHEMBL ID404431
CHEMBL ID221773
CHEMBL ID578577
CHEMBL ID1197433
CHEMBL ID580910
SCHEMBL ID13951812
SCHEMBL ID4547841
SCHEMBL ID11379522
SCHEMBL ID12612733
SCHEMBL ID10307589
CHEBI ID136054
MeSH IDM0472074

Synonyms (40)

Synonym
arterolane
oz277
arterolano
rbx11160
CHEBI:136054
rbx-11160
oz 277
n-(2-amino-2-methylpropyl)-2-[(1s,4s)-dispiro[cyclohexane-1,3'-[1,2,4]trioxolane-5',2''-tricyclo[3.3.1.1(3,7)]decan]-4-yl]acetamide
664338-39-0
arterolanum
CHEMBL404431
CHEMBL221773
oz-277
CHEMBL578577
CHEMBL1197433
3n1tn351vb ,
oz277 cpd
rbx 11160
unii-3n1tn351vb
arterolane [inn]
NCGC00274173-01
arterolane [who-dd]
dispiro(cyclohexane-1,3'-(1,2,4)trioxolane-5',2''-tricyclo(3.3.1.13,7)decane)-4-acetamide, n-(2-amino-2-methylpropyl)-, cis-
SCHEMBL13951812
SCHEMBL4547841
SCHEMBL11379522
SCHEMBL12612733
SCHEMBL10307589
CHEMBL580910
CS-0002648
HY-10852
VXYZBLXGCYNIHP-BBMJWGJISA-N
VXYZBLXGCYNIHP-CAGINOIPSA-N
n-(2-amino-2-methylpropyl)-2-((1r,3r,4''s,5r,5's,7r)-dispiro[adamantane-2,3'-[1,2,4]trioxolane-5',1''-cyclohexan]-4''-yl)acetamide
DTXSID50985095
oz 277;rbx 11160
AT25294
MS-26573
n-(2-amino-2-methylpropyl)-2-{dispiro[adamantane-2,2'-[1,3,5]trioxolane-4',1''-cyclohexane]-4''-yl}acetamide
AKOS040741167

Bioassays (128)

Assay IDTitleYearJournalArticle
AID728700Antimalarial activity against chloroquine-sensitive Plasmodium falciparum NF54 infected mouse assessed as reduction in parasitemia at 30 mg/kg, po measured on day 3 postinfection relative to control2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
ISSN: 1520-4804
Comparative antimalarial activities and ADME profiles of ozonides (1,2,4-trioxolanes) OZ277, OZ439, and their 1,2-dioxolane, 1,2,4-trioxane, and 1,2,4,5-tetraoxane isosteres.
AID520092Induction of heme alkylation of Fe(II) heme assessed as loss of heme at 10 uM in presence of 50% ACN-H2O with excess sodium dithionite under argon at 20 degC by spectrophotometry2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
ISSN: 0066-4804
Relationship between antimalarial activity and heme alkylation for spiro- and dispiro-1,2,4-trioxolane antimalarials.
AID1457833Antiplasmodial activity against Plasmodium falciparum Cam3.2_rev infected in human RBC assessed as time required to reduce early ring stage parasite viability by 50% by SYTO 61-staining-based flow cytometry2017Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14
ISSN: 1520-4804
Enantioselective Synthesis and in Vivo Evaluation of Regioisomeric Analogues of the Antimalarial Arterolane.
AID422400Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB 9002009Journal of natural products, Feb-27, Volume: 72, Issue:2
ISSN: 1520-6025
The marine sponge Diacarnus bismarckensis as a source of peroxiterpene inhibitors of Trypanosoma brucei, the causative agent of sleeping sickness.
AID366932Antiplasmodial activity as survival in Plasmodium berghei ANKA infected BALB/c mice (Mus musculus) at 30 mg/kg peroral dose2009Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
ISSN: 1520-4804
Malaria-infected mice are cured by a single oral dose of new dimeric trioxane sulfones which are also selectively and powerfully cytotoxic to cancer cells.
AID341601Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB9002007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
ISSN: 0066-4804
Peroxide bond-dependent antiplasmodial specificity of artemisinin and OZ277 (RBx11160).
AID572089Antimalarial activity against Plasmodium falciparum NF54 by [3H]hypoxanthine incorporation assay in presence of 2,2,6,6,-tetramethyl-1-piperidinyloxy2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
ISSN: 1098-6596
Probing the antimalarial mechanism of artemisinin and OZ277 (arterolane) with nonperoxidic isosteres and nitroxyl radicals.
AID560761Stability of compound in presence of oxyhemoglobin assessed as pseudo-first order degradation rate constant at 10 uM at 20degC over 24 hrs2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
ISSN: 1098-6596
Stability of peroxide antimalarials in the presence of human hemoglobin.
AID1777173Intrinsic clearance in mouse liver microsome by LC-MS/MS analysis2021ACS medicinal chemistry letters, Jul-08, Volume: 12, Issue:7
ISSN: 1948-5875
Enantioselective Synthesis and Profiling of Potent, Nonlinear Analogues of Antimalarial Tetraoxanes E209 and N205.
AID572078Antimalarial activity against Plasmodium falciparum NF54 by [3H]hypoxanthine incorporation assay in presence of 1:1 ratio of compound to 4-oxo-2,2,6,6,-tetramethyl-1-piperidinyloxy2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
ISSN: 1098-6596
Probing the antimalarial mechanism of artemisinin and OZ277 (arterolane) with nonperoxidic isosteres and nitroxyl radicals.
AID572074Antimalarial activity against Plasmodium falciparum NF54 by [3H]hypoxanthine incorporation assay in presence of 3:1 ratio of compound to 4-hydroxy-2,2,6,6,-tetramethyl-1-piperidinyloxy2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
ISSN: 1098-6596
Probing the antimalarial mechanism of artemisinin and OZ277 (arterolane) with nonperoxidic isosteres and nitroxyl radicals.
AID1457817Antiplasmodial activity against Plasmodium berghei infected in Swiss Webster mouse assessed as cure rate at 4 mg/kg/day administered for 4 days via oral gavage starting at 1 hr post infection measured after 30 days relative to control2017Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14
ISSN: 1520-4804
Enantioselective Synthesis and in Vivo Evaluation of Regioisomeric Analogues of the Antimalarial Arterolane.
AID341600Antiplasmodial activity against Plasmodium falciparum NF542007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
ISSN: 0066-4804
Peroxide bond-dependent antiplasmodial specificity of artemisinin and OZ277 (RBx11160).
AID1457810Antiplasmodial activity against Plasmodium falciparum Cam3.2 infected in human RBC assessed as time required to reduce early ring stage parasite viability by 50% by SYTO 61-staining-based flow cytometry2017Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14
ISSN: 1520-4804
Enantioselective Synthesis and in Vivo Evaluation of Regioisomeric Analogues of the Antimalarial Arterolane.
AID572091Antimalarial activity against Plasmodium falciparum K1 by [3H]hypoxanthine incorporation assay2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
ISSN: 1098-6596
Probing the antimalarial mechanism of artemisinin and OZ277 (arterolane) with nonperoxidic isosteres and nitroxyl radicals.
AID572084Antimalarial activity against Plasmodium falciparum NF54 by [3H]hypoxanthine incorporation assay in presence of deoxyartemisinin2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
ISSN: 1098-6596
Probing the antimalarial mechanism of artemisinin and OZ277 (arterolane) with nonperoxidic isosteres and nitroxyl radicals.
AID1457816Antiplasmodial activity against Plasmodium berghei infected in Swiss Webster mouse assessed as increase in cure rate administered for 4 days via oral gavage starting at 1 hr post infection measured after 30 days2017Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14
ISSN: 1520-4804
Enantioselective Synthesis and in Vivo Evaluation of Regioisomeric Analogues of the Antimalarial Arterolane.
AID1625265Antimalarial activity against GFP-transfected Plasmodium berghei ANKA infected in mouse assessed as reduction in parasitemia at 30 mg/kg, po administered on day 1 post infection measured on day 3 post infection2016Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12
ISSN: 1520-4804
Antimalarial Chemotherapy: Natural Product Inspired Development of Preclinical and Clinical Candidates with Diverse Mechanisms of Action.
AID728701Antimalarial activity against chloroquine-sensitive Plasmodium falciparum NF54 infected in mouse at 30 mg/kg, po2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
ISSN: 1520-4804
Comparative antimalarial activities and ADME profiles of ozonides (1,2,4-trioxolanes) OZ277, OZ439, and their 1,2-dioxolane, 1,2,4-trioxane, and 1,2,4,5-tetraoxane isosteres.
AID572081Antimalarial activity against Plasmodium falciparum NF54 by [3H]hypoxanthine incorporation assay in presence of 1:1 ratio of compound to 2,2,6,6,-tetramethyl-1-piperidinyloxy2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
ISSN: 1098-6596
Probing the antimalarial mechanism of artemisinin and OZ277 (arterolane) with nonperoxidic isosteres and nitroxyl radicals.
AID572075Antimalarial activity against Plasmodium falciparum NF54 by [3H]hypoxanthine incorporation assay in presence of 1:1 ratio of compound to 4-hydroxy-2,2,6,6,-tetramethyl-1-piperidinyloxy2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
ISSN: 1098-6596
Probing the antimalarial mechanism of artemisinin and OZ277 (arterolane) with nonperoxidic isosteres and nitroxyl radicals.
AID560760Stability of compound in presence water assessed as pseudo-first order degradation rate constant at 10 uM at 20degC over 24 hrs2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
ISSN: 1098-6596
Stability of peroxide antimalarials in the presence of human hemoglobin.
AID728696Dissociation constant, pKa of the compound2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
ISSN: 1520-4804
Comparative antimalarial activities and ADME profiles of ozonides (1,2,4-trioxolanes) OZ277, OZ439, and their 1,2-dioxolane, 1,2,4-trioxane, and 1,2,4,5-tetraoxane isosteres.
AID1625266Oral bioavailability in rat at 3 mg/kg2016Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12
ISSN: 1520-4804
Antimalarial Chemotherapy: Natural Product Inspired Development of Preclinical and Clinical Candidates with Diverse Mechanisms of Action.
AID1457815Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum W2 infected in human RBC after 48 hrs by YOYO-1 staining-based flow cytometry method2017Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14
ISSN: 1520-4804
Enantioselective Synthesis and in Vivo Evaluation of Regioisomeric Analogues of the Antimalarial Arterolane.
AID572083Antimalarial activity against Plasmodium falciparum NF54 by [3H]hypoxanthine incorporation assay in presence of carbaOZ2772010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
ISSN: 1098-6596
Probing the antimalarial mechanism of artemisinin and OZ277 (arterolane) with nonperoxidic isosteres and nitroxyl radicals.
AID447027Antimalarial activity against Plasmodium falciparum NF542009Bioorganic & medicinal chemistry letters, Oct-01, Volume: 19, Issue:19
ISSN: 1464-3405
Synthesis and in vitro DMPK profiling of a 1,2-dioxolane-based library with activity against Plasmodium falciparum.
AID632148Binding affinity to Plasmodium falciparum calcium-transporting ATPase2011Journal of medicinal chemistry, Dec-08, Volume: 54, Issue:23
ISSN: 1520-4804
Investigating the antimalarial action of 1,2,4-trioxolanes with fluorescent chemical probes.
AID520094Induction of heme alkylation of Fe(II) heme assessed as adduct A472 absorbance change at completion of reaction at 10 uM in presence of 50% ACN-H2O with excess sodium dithionite under argon at 20 degC by spectrophotometry2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
ISSN: 0066-4804
Relationship between antimalarial activity and heme alkylation for spiro- and dispiro-1,2,4-trioxolane antimalarials.
AID572082Antimalarial activity against Plasmodium falciparum NF54 by [3H]hypoxanthine incorporation assay in presence of 1:3 ratio of compound to 2,2,6,6,-tetramethyl-1-piperidinyloxy2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
ISSN: 1098-6596
Probing the antimalarial mechanism of artemisinin and OZ277 (arterolane) with nonperoxidic isosteres and nitroxyl radicals.
AID320102Distribution coefficient, log D of the compound2008Bioorganic & medicinal chemistry letters, Mar-01, Volume: 18, Issue:5
ISSN: 1464-3405
Characterization of the two major CYP450 metabolites of ozonide (1,2,4-trioxolane) OZ277.
AID1625264Antimalarial activity against chloroquine-resistant Plasmodium falciparum K1 after 24 hrs in presence of hypoxanthine2016Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12
ISSN: 1520-4804
Antimalarial Chemotherapy: Natural Product Inspired Development of Preclinical and Clinical Candidates with Diverse Mechanisms of Action.
AID620219Induction of oxyl radical formation from reaction with ferrous salt in the presence of 2,2,6,6-tetramethyl-1-piperidine-1-oxyl after 24 hrs by spin-trapping and LC/MS analysis2011Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19
ISSN: 1520-4804
Comparison of the reactivity of antimalarial 1,2,4,5-tetraoxanes with 1,2,4-trioxolanes in the presence of ferrous iron salts, heme, and ferrous iron salts/phosphatidylcholine.
AID341607Antimicrobial activity against Babesia divergens 42012007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
ISSN: 0066-4804
Peroxide bond-dependent antiplasmodial specificity of artemisinin and OZ277 (RBx11160).
AID728702Antimalarial activity against chloroquine-resistant Plasmodium falciparum K12013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
ISSN: 1520-4804
Comparative antimalarial activities and ADME profiles of ozonides (1,2,4-trioxolanes) OZ277, OZ439, and their 1,2-dioxolane, 1,2,4-trioxane, and 1,2,4,5-tetraoxane isosteres.
AID341606Antimicrobial activity against Babesia divergens 1903B2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
ISSN: 0066-4804
Peroxide bond-dependent antiplasmodial specificity of artemisinin and OZ277 (RBx11160).
AID572080Antimalarial activity against Plasmodium falciparum NF54 by [3H]hypoxanthine incorporation assay in presence of 3:1 ratio of compound to 2,2,6,6,-tetramethyl-1-piperidinyloxy2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
ISSN: 1098-6596
Probing the antimalarial mechanism of artemisinin and OZ277 (arterolane) with nonperoxidic isosteres and nitroxyl radicals.
AID341602Antitrypanosomal activity against Trypanosoma cruzi Tulahuen C42007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
ISSN: 0066-4804
Peroxide bond-dependent antiplasmodial specificity of artemisinin and OZ277 (RBx11160).
AID572069Antimalarial activity against Plasmodium falciparum NF54 by [3H]hypoxanthine incorporation assay in presence of 1:1 ratio of compound to 4-amino-2,2,6,6,-tetramethyl-1-piperidinyloxy2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
ISSN: 1098-6596
Probing the antimalarial mechanism of artemisinin and OZ277 (arterolane) with nonperoxidic isosteres and nitroxyl radicals.
AID572068Antimalarial activity against Plasmodium falciparum NF54 by [3H]hypoxanthine incorporation assay in presence of 3:1 ratio of compound to 4-amino-2,2,6,6,-tetramethyl-1-piperidinyloxy2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
ISSN: 1098-6596
Probing the antimalarial mechanism of artemisinin and OZ277 (arterolane) with nonperoxidic isosteres and nitroxyl radicals.
AID632150Antimalarial activity against Plasmodium falciparum K1 infected in human A-positive type erythrocytes after 72 hrs by SRB assay2011Journal of medicinal chemistry, Dec-08, Volume: 54, Issue:23
ISSN: 1520-4804
Investigating the antimalarial action of 1,2,4-trioxolanes with fluorescent chemical probes.
AID447026Antimalarial activity against Plasmodium falciparum K12009Bioorganic & medicinal chemistry letters, Oct-01, Volume: 19, Issue:19
ISSN: 1464-3405
Synthesis and in vitro DMPK profiling of a 1,2-dioxolane-based library with activity against Plasmodium falciparum.
AID728692AUC (0 to 24 hrs) in mouse at 30 mg/kg, po by LC-MS analysis2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
ISSN: 1520-4804
Comparative antimalarial activities and ADME profiles of ozonides (1,2,4-trioxolanes) OZ277, OZ439, and their 1,2-dioxolane, 1,2,4-trioxane, and 1,2,4,5-tetraoxane isosteres.
AID572073Antimalarial activity against Plasmodium falciparum NF54 by [3H]hypoxanthine incorporation assay in presence of 1:3 ratio of compound to 4-carboxy-2,2,6,6,-tetramethyl-1-piperidinyloxy2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
ISSN: 1098-6596
Probing the antimalarial mechanism of artemisinin and OZ277 (arterolane) with nonperoxidic isosteres and nitroxyl radicals.
AID728699Antimalarial activity against chloroquine-sensitive Plasmodium falciparum NF54 infected mouse assessed as survival at 30 mg/kg, po2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
ISSN: 1520-4804
Comparative antimalarial activities and ADME profiles of ozonides (1,2,4-trioxolanes) OZ277, OZ439, and their 1,2-dioxolane, 1,2,4-trioxane, and 1,2,4,5-tetraoxane isosteres.
AID572086Antimalarial activity against Plasmodium falciparum NF54 by [3H]hypoxanthine incorporation assay in presence of 4-carboxy-2,2,6,6,-tetramethyl-1-piperidinyloxy2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
ISSN: 1098-6596
Probing the antimalarial mechanism of artemisinin and OZ277 (arterolane) with nonperoxidic isosteres and nitroxyl radicals.
AID572090Antimalarial activity against Plasmodium falciparum NF54 by [3H]hypoxanthine incorporation assay2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
ISSN: 1098-6596
Probing the antimalarial mechanism of artemisinin and OZ277 (arterolane) with nonperoxidic isosteres and nitroxyl radicals.
AID572067Antimalarial activity against Plasmodium falciparum NF54 by [3H]hypoxanthine incorporation assay in presence 1:3 ratio of compound to deoxyartemisinin2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
ISSN: 1098-6596
Probing the antimalarial mechanism of artemisinin and OZ277 (arterolane) with nonperoxidic isosteres and nitroxyl radicals.
AID572088Antimalarial activity against Plasmodium falciparum NF54 by [3H]hypoxanthine incorporation assay in presence of 4-oxo-2,2,6,6,-tetramethyl-1-piperidinyloxy2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
ISSN: 1098-6596
Probing the antimalarial mechanism of artemisinin and OZ277 (arterolane) with nonperoxidic isosteres and nitroxyl radicals.
AID572087Antimalarial activity against Plasmodium falciparum NF54 by [3H]hypoxanthine incorporation assay in presence of 4-hydroxy-2,2,6,6,-tetramethyl-1-piperidinyloxy2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
ISSN: 1098-6596
Probing the antimalarial mechanism of artemisinin and OZ277 (arterolane) with nonperoxidic isosteres and nitroxyl radicals.
AID728695Lipophilicity, log D of the compound at pH 7.42013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
ISSN: 1520-4804
Comparative antimalarial activities and ADME profiles of ozonides (1,2,4-trioxolanes) OZ277, OZ439, and their 1,2-dioxolane, 1,2,4-trioxane, and 1,2,4,5-tetraoxane isosteres.
AID572066Antimalarial activity against Plasmodium falciparum NF54 by [3H]hypoxanthine incorporation assay in presence 1:1 ratio of compound to deoxyartemisinin2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
ISSN: 1098-6596
Probing the antimalarial mechanism of artemisinin and OZ277 (arterolane) with nonperoxidic isosteres and nitroxyl radicals.
AID728691Plasma concentration in Swiss outbred mouse at 30 mg/kg, po at 24 hrs by LC-MS analysis2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
ISSN: 1520-4804
Comparative antimalarial activities and ADME profiles of ozonides (1,2,4-trioxolanes) OZ277, OZ439, and their 1,2-dioxolane, 1,2,4-trioxane, and 1,2,4,5-tetraoxane isosteres.
AID341604Antimicrobial activity against Giardia duodenalis WB2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
ISSN: 0066-4804
Peroxide bond-dependent antiplasmodial specificity of artemisinin and OZ277 (RBx11160).
AID572071Antimalarial activity against Plasmodium falciparum NF54 by [3H]hypoxanthine incorporation assay in presence of 3:1 ratio of compound to 4-carboxy-2,2,6,6,-tetramethyl-1-piperidinyloxy2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
ISSN: 1098-6596
Probing the antimalarial mechanism of artemisinin and OZ277 (arterolane) with nonperoxidic isosteres and nitroxyl radicals.
AID728694Intrinsic clearance in mouse liver microsomes at 1 uM after 60 mins by LC-MS analysis2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
ISSN: 1520-4804
Comparative antimalarial activities and ADME profiles of ozonides (1,2,4-trioxolanes) OZ277, OZ439, and their 1,2-dioxolane, 1,2,4-trioxane, and 1,2,4,5-tetraoxane isosteres.
AID572092Antimalarial activity against Plasmodium falciparum NF54 by [3H]hypoxanthine incorporation assay in presence 1:1 ratio of compound to carbaOZ2772010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
ISSN: 1098-6596
Probing the antimalarial mechanism of artemisinin and OZ277 (arterolane) with nonperoxidic isosteres and nitroxyl radicals.
AID1777174Intrinsic clearance in mouse liver microsome assessed as half life by LC-MS/MS analysis2021ACS medicinal chemistry letters, Jul-08, Volume: 12, Issue:7
ISSN: 1948-5875
Enantioselective Synthesis and Profiling of Potent, Nonlinear Analogues of Antimalarial Tetraoxanes E209 and N205.
AID572085Antimalarial activity against Plasmodium falciparum NF54 by [3H]hypoxanthine incorporation assay in presence of 4-amino-2,2,6,6,-tetramethyl-1-piperidinyloxy2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
ISSN: 1098-6596
Probing the antimalarial mechanism of artemisinin and OZ277 (arterolane) with nonperoxidic isosteres and nitroxyl radicals.
AID341603Antileishmanial activity against Leishmania donovani MHOM-ET-67/L82 amastigotes by axenic assay2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
ISSN: 0066-4804
Peroxide bond-dependent antiplasmodial specificity of artemisinin and OZ277 (RBx11160).
AID430464Induction of heme alkylation measured within 30 seconds by visible spectrophotometry2009Bioorganic & medicinal chemistry letters, Aug-15, Volume: 19, Issue:16
ISSN: 1464-3405
Spiroadamantyl 1,2,4-trioxolane, 1,2,4-trioxane, and 1,2,4-trioxepane pairs: relationship between peroxide bond iron(II) reactivity, heme alkylation efficiency, and antimalarial activity.
AID366936Antiplasmodial activity as reduced parasitaemia in Plasmodium berghei ANKA infected BALB/c mice (Mus musculus) at 30 mg/kg peroral dose2009Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
ISSN: 1520-4804
Malaria-infected mice are cured by a single oral dose of new dimeric trioxane sulfones which are also selectively and powerfully cytotoxic to cancer cells.
AID728698Antimalarial activity against chloroquine-sensitive Plasmodium falciparum NF54 infected mouse assessed as cured animal at 30 mg/kg, po measured on day 30 postinfection2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
ISSN: 1520-4804
Comparative antimalarial activities and ADME profiles of ozonides (1,2,4-trioxolanes) OZ277, OZ439, and their 1,2-dioxolane, 1,2,4-trioxane, and 1,2,4,5-tetraoxane isosteres.
AID341612Inhibition of Plasmodium falciparum ATP62007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
ISSN: 0066-4804
Peroxide bond-dependent antiplasmodial specificity of artemisinin and OZ277 (RBx11160).
AID320101Antimalarial activity against Plasmodium falciparum K12008Bioorganic & medicinal chemistry letters, Mar-01, Volume: 18, Issue:5
ISSN: 1464-3405
Characterization of the two major CYP450 metabolites of ozonide (1,2,4-trioxolane) OZ277.
AID572076Antimalarial activity against Plasmodium falciparum NF54 by [3H]hypoxanthine incorporation assay in presence of 1:3 ratio of compound to 4-hydroxy-2,2,6,6,-tetramethyl-1-piperidinyloxy2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
ISSN: 1098-6596
Probing the antimalarial mechanism of artemisinin and OZ277 (arterolane) with nonperoxidic isosteres and nitroxyl radicals.
AID1457811Half life in mouse liver microsomes2017Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14
ISSN: 1520-4804
Enantioselective Synthesis and in Vivo Evaluation of Regioisomeric Analogues of the Antimalarial Arterolane.
AID572093Antimalarial activity against Plasmodium falciparum NF54 by [3H]hypoxanthine incorporation assay in presence 3:1 ratio of compound to carbaOZ2772010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
ISSN: 1098-6596
Probing the antimalarial mechanism of artemisinin and OZ277 (arterolane) with nonperoxidic isosteres and nitroxyl radicals.
AID572070Antimalarial activity against Plasmodium falciparum NF54 by [3H]hypoxanthine incorporation assay in presence of 1:3 ratio of compound to 4-amino-2,2,6,6,-tetramethyl-1-piperidinyloxy2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
ISSN: 1098-6596
Probing the antimalarial mechanism of artemisinin and OZ277 (arterolane) with nonperoxidic isosteres and nitroxyl radicals.
AID1457812Intrinsic clearance in mouse liver microsomes assessed per mg of protein2017Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14
ISSN: 1520-4804
Enantioselective Synthesis and in Vivo Evaluation of Regioisomeric Analogues of the Antimalarial Arterolane.
AID341599Antiplasmodial activity against Plasmodium falciparum K12007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
ISSN: 0066-4804
Peroxide bond-dependent antiplasmodial specificity of artemisinin and OZ277 (RBx11160).
AID560762Stability of compound in presence of methoxyhemoglobin assessed as pseudo-first order degradation rate constant at 10 uM at 20degC over 24 hrs2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
ISSN: 1098-6596
Stability of peroxide antimalarials in the presence of human hemoglobin.
AID772516Antimalarial activity against mature gametocytic stage of Plasmodium falciparum assessed as inhibition of mature gamete exflagellation at 10 uM incubated for 24 hrs prior to exflagellation induction at 21 degC measured after 20 mins by microscopic analysi2013Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20
ISSN: 1520-4804
Using genetic methods to define the targets of compounds with antimalarial activity.
AID728693Half life in mouse whole blood2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
ISSN: 1520-4804
Comparative antimalarial activities and ADME profiles of ozonides (1,2,4-trioxolanes) OZ277, OZ439, and their 1,2-dioxolane, 1,2,4-trioxane, and 1,2,4,5-tetraoxane isosteres.
AID341605Antimicrobial activity against Giardia duodenalis G12007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
ISSN: 0066-4804
Peroxide bond-dependent antiplasmodial specificity of artemisinin and OZ277 (RBx11160).
AID572079Antimalarial activity against Plasmodium falciparum NF54 by [3H]hypoxanthine incorporation assay in presence of 1:3 ratio of compound to 4-oxo-2,2,6,6,-tetramethyl-1-piperidinyloxy2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
ISSN: 1098-6596
Probing the antimalarial mechanism of artemisinin and OZ277 (arterolane) with nonperoxidic isosteres and nitroxyl radicals.
AID1457832Metabolic stability in mouse liver microsomes in absence of NADPH2017Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14
ISSN: 1520-4804
Enantioselective Synthesis and in Vivo Evaluation of Regioisomeric Analogues of the Antimalarial Arterolane.
AID1457818Antiplasmodial activity against Plasmodium berghei infected in Swiss Webster mouse assessed as cure rate at 1 mg/kg/day administered for 4 days via oral gavage starting at 1 hr post infection measured after 30 days relative to control2017Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14
ISSN: 1520-4804
Enantioselective Synthesis and in Vivo Evaluation of Regioisomeric Analogues of the Antimalarial Arterolane.
AID728697Partition coefficient, log P of the compound2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
ISSN: 1520-4804
Comparative antimalarial activities and ADME profiles of ozonides (1,2,4-trioxolanes) OZ277, OZ439, and their 1,2-dioxolane, 1,2,4-trioxane, and 1,2,4,5-tetraoxane isosteres.
AID341598Antimicrobial activity against Neospora caninum up to 1 ug/ml2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
ISSN: 0066-4804
Peroxide bond-dependent antiplasmodial specificity of artemisinin and OZ277 (RBx11160).
AID1777163Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum W2 incubated for 72 hrs by spectrophotometry based parasite lactate dehydrogenase assay2021ACS medicinal chemistry letters, Jul-08, Volume: 12, Issue:7
ISSN: 1948-5875
Enantioselective Synthesis and Profiling of Potent, Nonlinear Analogues of Antimalarial Tetraoxanes E209 and N205.
AID1457814Kinetic solubility of the compound in PBS at pH 7.42017Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14
ISSN: 1520-4804
Enantioselective Synthesis and in Vivo Evaluation of Regioisomeric Analogues of the Antimalarial Arterolane.
AID572077Antimalarial activity against Plasmodium falciparum NF54 by [3H]hypoxanthine incorporation assay in presence of 3:1 ratio of compound to 4-oxo-2,2,6,6,-tetramethyl-1-piperidinyloxy2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
ISSN: 1098-6596
Probing the antimalarial mechanism of artemisinin and OZ277 (arterolane) with nonperoxidic isosteres and nitroxyl radicals.
AID1457820Antiplasmodial activity against Plasmodium berghei infected in Swiss Webster mouse assessed as cure rate at 10 mg/kg/day administered for 4 days via oral gavage starting at 1 hr post infection measured after 30 days relative to control2017Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14
ISSN: 1520-4804
Enantioselective Synthesis and in Vivo Evaluation of Regioisomeric Analogues of the Antimalarial Arterolane.
AID572064Antimalarial activity against Plasmodium falciparum NF54 by [3H]hypoxanthine incorporation assay in presence 1:3 ratio of compound to carbaOZ2772010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
ISSN: 1098-6596
Probing the antimalarial mechanism of artemisinin and OZ277 (arterolane) with nonperoxidic isosteres and nitroxyl radicals.
AID520093Antimalarial activity against chloroquine-resistant Plasmodium falciparum K12008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
ISSN: 0066-4804
Relationship between antimalarial activity and heme alkylation for spiro- and dispiro-1,2,4-trioxolane antimalarials.
AID572072Antimalarial activity against Plasmodium falciparum NF54 by [3H]hypoxanthine incorporation assay in presence of 1:1 ratio of compound to 4-carboxy-2,2,6,6,-tetramethyl-1-piperidinyloxy2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
ISSN: 1098-6596
Probing the antimalarial mechanism of artemisinin and OZ277 (arterolane) with nonperoxidic isosteres and nitroxyl radicals.
AID572065Antimalarial activity against Plasmodium falciparum NF54 by [3H]hypoxanthine incorporation assay in presence 3:1 ratio of compound to deoxyartemisinin2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
ISSN: 1098-6596
Probing the antimalarial mechanism of artemisinin and OZ277 (arterolane) with nonperoxidic isosteres and nitroxyl radicals.
AID1457819Antiplasmodial activity against Plasmodium berghei infected in Swiss Webster mouse assessed as cure rate at 6 mg/kg/day administered for 4 days via oral gavage starting at 1 hr post infection measured after 30 days relative to control2017Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14
ISSN: 1520-4804
Enantioselective Synthesis and in Vivo Evaluation of Regioisomeric Analogues of the Antimalarial Arterolane.
AID748927Half life in Sprague-Dawley rat at 3 mg/kg, iv2013Bioorganic & medicinal chemistry letters, May-15, Volume: 23, Issue:10
ISSN: 1464-3405
Recent advances in malaria drug discovery.
AID1508612NCATS Parallel Artificial Membrane Permeability Assay (PAMPA) Profiling2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
ISSN: 1464-3391
Highly predictive and interpretable models for PAMPA permeability.
AID1508591NCATS Rat Liver Microsome Stability Profiling2020Scientific reports, 11-26, Volume: 10, Issue:1
ISSN: 2045-2322
Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
AID1645848NCATS Kinetic Aqueous Solubility Profiling2019Bioorganic & medicinal chemistry, 07-15, Volume: 27, Issue:14
ISSN: 1464-3391
Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
AID1873043Antimalarial activity against chloroquine sensitive Plasmodium falciparum NF54 assessed as inhibition of parasite growth by [3H]-hypoxanthine incorporation assay2022European journal of medicinal chemistry, Jul-05, Volume: 237ISSN: 1768-3254Spiral molecules with antimalarial activities: A review.
AID1496712Antimalarial activity against Plasmodium berghei infected in mouse assessed as reduction in parasitemia at 30 mg/kg, po administered as single dose measured on day 3 relative to control2018Bioorganic & medicinal chemistry, 07-15, Volume: 26, Issue:11
ISSN: 1464-3391
Synthesis and profiling of benzylmorpholine 1,2,4,5-tetraoxane analogue N205: Towards tetraoxane scaffolds with potential for single dose cure of malaria.
AID1873042Antimalarial activity against chloroquine resistant Plasmodium falciparum K1 assessed as inhibition of parasite growth by [3H]-hypoxanthine incorporation assay2022European journal of medicinal chemistry, Jul-05, Volume: 237ISSN: 1768-3254Spiral molecules with antimalarial activities: A review.
AID1496713Antimalarial activity against Plasmodium berghei infected in mouse assessed as mouse mean survival days at 30 mg/kg, po administered as single dose2018Bioorganic & medicinal chemistry, 07-15, Volume: 26, Issue:11
ISSN: 1464-3391
Synthesis and profiling of benzylmorpholine 1,2,4,5-tetraoxane analogue N205: Towards tetraoxane scaffolds with potential for single dose cure of malaria.
AID1440472In vivo antimalarial activity against Plasmodium berghei infected in albino mouse assessed as as protection against infection at 100 mg/kg, po single dose administered 48 hrs prior to infection2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
ISSN: 1520-4804
Structure-Activity Relationship of the Antimalarial Ozonide Artefenomel (OZ439).
AID1440469Plasma concentration in FVB mouse at 30 mg/kg, administered through oral gavage as single dose measured after 48 hrs post dose by LC-MS analysis2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
ISSN: 1520-4804
Structure-Activity Relationship of the Antimalarial Ozonide Artefenomel (OZ439).
AID1440463Intrinsic clearance in mouse liver microsomes at 1 uM by LC/MS analysis2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
ISSN: 1520-4804
Structure-Activity Relationship of the Antimalarial Ozonide Artefenomel (OZ439).
AID1440475In vivo antimalarial activity against Plasmodium berghei infected in albino mouse assessed as mouse survival at 100 mg/kg, po single dose administered 96 hrs prior to infection (Rvb = 6 to 7 days)2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
ISSN: 1520-4804
Structure-Activity Relationship of the Antimalarial Ozonide Artefenomel (OZ439).
AID1276198Stability in human blood after 240 mins by LC/MS analysis2015ACS medicinal chemistry letters, Nov-12, Volume: 6, Issue:11
ISSN: 1948-5875
Trioxolane-Mediated Delivery of Mefloquine Limits Brain Exposure in a Mouse Model of Malaria.
AID1440464Intrinsic clearance in rat liver microsomes at 1 uM by LC/MS analysis2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
ISSN: 1520-4804
Structure-Activity Relationship of the Antimalarial Ozonide Artefenomel (OZ439).
AID1440482In vivo antimalarial activity against GFP-transfected Plasmodium berghei ANKA infected in mouse assessed as mean survival days at 30 mg/kg, po administered as single dose measured after 30 days post infection by flow cytometric analysis2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
ISSN: 1520-4804
Structure-Activity Relationship of the Antimalarial Ozonide Artefenomel (OZ439).
AID1440468Cmax in FVB mouse at 30 mg/kg, administered through oral gavage as single dose by LC-MS analysis2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
ISSN: 1520-4804
Structure-Activity Relationship of the Antimalarial Ozonide Artefenomel (OZ439).
AID1440483In vivo antimalarial activity against GFP-transfected Plasmodium berghei ANKA infected in mouse assessed as parasitemia cured mouse at 30 mg/kg, po administered as single dose measured after 30 days post infection by flow cytometric analysis2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
ISSN: 1520-4804
Structure-Activity Relationship of the Antimalarial Ozonide Artefenomel (OZ439).
AID1440457Antimalarial activity against chloroquine-resistant Plasmodium falciparum K1 assessed as reduction in [3H]-hypoxanthine incorporation preincubated for 24 hrs followed by [3H]-hypoxanthine addition measured after 18 hrs by liquid scintillation counting2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
ISSN: 1520-4804
Structure-Activity Relationship of the Antimalarial Ozonide Artefenomel (OZ439).
AID1440476In vivo antimalarial activity against Plasmodium berghei infected in albino mouse assessed as as protection against infection at 100 mg/kg, po single dose administered 96 hrs prior to infection2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
ISSN: 1520-4804
Structure-Activity Relationship of the Antimalarial Ozonide Artefenomel (OZ439).
AID1440462Intrinsic clearance in human liver microsomes at 1 uM by LC/MS analysis2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
ISSN: 1520-4804
Structure-Activity Relationship of the Antimalarial Ozonide Artefenomel (OZ439).
AID1276199Ratio of drug level in human blood to plasma2015ACS medicinal chemistry letters, Nov-12, Volume: 6, Issue:11
ISSN: 1948-5875
Trioxolane-Mediated Delivery of Mefloquine Limits Brain Exposure in a Mouse Model of Malaria.
AID1276196Stability in human plasma after 240 mins by LC/MS analysis2015ACS medicinal chemistry letters, Nov-12, Volume: 6, Issue:11
ISSN: 1948-5875
Trioxolane-Mediated Delivery of Mefloquine Limits Brain Exposure in a Mouse Model of Malaria.
AID1440477In vivo antimalarial activity against Plasmodium berghei infected in albino mouse assessed as fold change in mouse survival at 100 mg/kg, po single dose administered 72 hrs prior to infection relative to control2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
ISSN: 1520-4804
Structure-Activity Relationship of the Antimalarial Ozonide Artefenomel (OZ439).
AID1440458Antimalarial activity against chloroquine-sensitive Plasmodium falciparum NF54 assessed as reduction in [3H]-hypoxanthine incorporation preincubated for 24 hrs followed by [3H]-hypoxanthine addition measured after 18 hrs by liquid scintillation counting2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
ISSN: 1520-4804
Structure-Activity Relationship of the Antimalarial Ozonide Artefenomel (OZ439).
AID1440470In vivo antimalarial activity against Plasmodium berghei infected in albino mouse assessed as mouse survival at 100 mg/kg, po single dose administered 48 hrs prior to infection (Rvb = 6 to 7 days)2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
ISSN: 1520-4804
Structure-Activity Relationship of the Antimalarial Ozonide Artefenomel (OZ439).
AID1440466Kinetic solubility of the compound in water after 30 mins by nephelometric analysis2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
ISSN: 1520-4804
Structure-Activity Relationship of the Antimalarial Ozonide Artefenomel (OZ439).
AID1440465Intrinsic clearance in dog liver microsomes at 1 uM by LC/MS analysis2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
ISSN: 1520-4804
Structure-Activity Relationship of the Antimalarial Ozonide Artefenomel (OZ439).
AID1276195Antiplasmodium activity against Plasmodium falciparum W2 by flow cytometry2015ACS medicinal chemistry letters, Nov-12, Volume: 6, Issue:11
ISSN: 1948-5875
Trioxolane-Mediated Delivery of Mefloquine Limits Brain Exposure in a Mouse Model of Malaria.
AID1440471In vivo antimalarial activity against Plasmodium berghei infected in albino mouse assessed as mouse survival at 30 mg/kg, po single dose administered 24 hrs prior to infection (Rvb = 6 to 7 days)2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
ISSN: 1520-4804
Structure-Activity Relationship of the Antimalarial Ozonide Artefenomel (OZ439).
AID1440467AUC (0 to infinity) in FVB mouse at 30 mg/kg, administered through oral gavage as single dose by LC-MS analysis2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
ISSN: 1520-4804
Structure-Activity Relationship of the Antimalarial Ozonide Artefenomel (OZ439).
AID1440473In vivo antimalarial activity against Plasmodium berghei infected in albino mouse assessed as mouse survival at 100 mg/kg, po single dose administered 72 hrs prior to infection (Rvb = 6 to 7 days)2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
ISSN: 1520-4804
Structure-Activity Relationship of the Antimalarial Ozonide Artefenomel (OZ439).
AID1440474In vivo antimalarial activity against Plasmodium berghei infected in albino mouse assessed as as protection against infection at 100 mg/kg, po single dose administered 72 hrs prior to infection2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
ISSN: 1520-4804
Structure-Activity Relationship of the Antimalarial Ozonide Artefenomel (OZ439).
AID1440455In vivo antimalarial activity against Plasmodium berghei infected in albino mouse assessed as protection against infection at 30 mg/kg, po single dose administered 24 hrs prior to infection2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
ISSN: 1520-4804
Structure-Activity Relationship of the Antimalarial Ozonide Artefenomel (OZ439).
AID279859Inhibition of Plasmodium falciparum ATP6 expressed in Xenopus laevis oocytes2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
ISSN: 0066-4804
Mechanism of antimalarial action of the synthetic trioxolane RBX11160 (OZ277).
AID279860Antimalarial activity against Plasmodium falciparum NF54 within 48 hrs2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
ISSN: 0066-4804
Mechanism of antimalarial action of the synthetic trioxolane RBX11160 (OZ277).
AID279857Inhibition of rabbit muscle SERCA at 100 uM2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
ISSN: 0066-4804
Mechanism of antimalarial action of the synthetic trioxolane RBX11160 (OZ277).
AID279855Inhibition of Plasmodium falciparum ATP6 expressed in Xenopus laevis oocytes at 50 uM2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
ISSN: 0066-4804
Mechanism of antimalarial action of the synthetic trioxolane RBX11160 (OZ277).
AID279858Inhibition of Plasmodium falciparum HT expressed in Xenopus laevis oocytes assessed as D-[U-14C]glucose uptake at 50 uM2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
ISSN: 0066-4804
Mechanism of antimalarial action of the synthetic trioxolane RBX11160 (OZ277).
AID279861Abrogation of Plasmodium falciparum ATP6 inhibition expressed in Xenopus laevis oocytes at 10 uM in presence of 100 uM desferioxamine2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
ISSN: 0066-4804
Mechanism of antimalarial action of the synthetic trioxolane RBX11160 (OZ277).

Research

Studies (59)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's20 (33.90)29.6817
2010's32 (54.24)24.3611
2020's7 (11.86)2.80

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials10 (16.67%)5.53%
Reviews4 (6.67%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other46 (76.67%)84.16%
SubstanceStudiesClassesRolesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
fosmidomycinhydroxamic acid;
phosphonic acids
antimicrobial agent;
bacterial metabolite;
EC 1.1.1.267 (1-deoxy-D-xylulose-5-phosphate reductoisomerase) inhibitor
201620168.0low000010
b 844-39diarylmethane201720177.0low000010
pk 11195aromatic amide;
isoquinolines;
monocarboxylic acid amide;
monochlorobenzenes
antineoplastic agent201720205.3low000030
jtv519201720205.3high000030
albendazolearyl sulfide;
benzimidazoles;
benzimidazolylcarbamate fungicide;
carbamate ester
anthelminthic drug;
microtubule-destabilising agent;
tubulin modulator
2007200717.0low000100
alprazolamorganochlorine compound;
triazolobenzodiazepine
anticonvulsant;
anxiolytic drug;
GABA agonist;
muscle relaxant;
sedative;
xenobiotic
201720205.3low000030
amiodarone1-benzofurans;
aromatic ketone;
organoiodine compound;
tertiary amino compound
cardiovascular drug201720177.0low000010
dan 2163aromatic amide;
aromatic amine;
benzamides;
pyrrolidines;
sulfone
environmental contaminant;
second generation antipsychotic;
xenobiotic
201720205.3low000030
amlexanoxmonocarboxylic acid;
pyridochromene
anti-allergic agent;
anti-ulcer drug;
non-steroidal anti-inflammatory drug
201720205.3low000030
astemizolebenzimidazoles;
piperidines
anti-allergic agent;
anticoronaviral agent;
H1-receptor antagonist
201720205.3low000030
benzbromarone1-benzofurans;
aromatic ketone
uricosuric drug201720205.3low000030
bisindolylmaleimide i201720205.3low000030
bufexamacaromatic ether;
hydroxamic acid
antipyretic;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug
201720205.3low000030
cadralazineorganic molecular entity201720205.3low000030
carvedilolcarbazoles;
secondary alcohol;
secondary amino compound
alpha-adrenergic antagonist;
antihypertensive agent;
beta-adrenergic antagonist;
cardiovascular drug;
vasodilator agent
201920204.5low000020
cetirizineether;
monocarboxylic acid;
monochlorobenzenes;
piperazines
anti-allergic agent;
environmental contaminant;
H1-receptor antagonist;
xenobiotic
201920204.5low000020
chlorcyclizinediarylmethane201720205.3low000030
chloroquineaminoquinoline;
organochlorine compound;
secondary amino compound;
tertiary amino compound
anticoronaviral agent;
antimalarial;
antirheumatic drug;
autophagy inhibitor;
dermatologic drug
201320218.0low000031
ci 994acetamides;
benzamides;
substituted aniline
antineoplastic agent;
EC 3.5.1.98 (histone deacetylase) inhibitor
201720205.3low000030
cyclosporine201720205.5high000020
diclofenacamino acid;
aromatic amine;
dichlorobenzene;
monocarboxylic acid;
secondary amino compound
antipyretic;
drug allergen;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
environmental contaminant;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
xenobiotic
201720177.0low000010
fenbendazolearyl sulfide;
benzimidazoles;
carbamate ester
antinematodal drug201720205.3low000030
berotekresorcinols;
secondary alcohol;
secondary amino compound
beta-adrenergic agonist;
bronchodilator agent;
sympathomimetic agent;
tocolytic agent
201720177.0low000010
furafyllineoxopurine201820186.0low000010
go 6976indolocarbazole;
organic heterohexacyclic compound
EC 2.7.11.13 (protein kinase C) inhibitor201720205.3low000030
haloperidolaromatic ketone;
hydroxypiperidine;
monochlorobenzenes;
organofluorine compound;
tertiary alcohol
antidyskinesia agent;
antiemetic;
dopaminergic antagonist;
first generation antipsychotic;
serotonergic antagonist
201720205.3low000030
miltefosinephosphocholines;
phospholipid
anti-inflammatory agent;
anticoronaviral agent;
antifungal agent;
antineoplastic agent;
antiprotozoal drug;
apoptosis inducer;
immunomodulator;
protein kinase inhibitor
2007200717.0low000100
homochlorocyclizinediarylmethane201720205.3low000030
hydroxyzinehydroxyether;
monochlorobenzenes;
N-alkylpiperazine
anticoronaviral agent;
antipruritic drug;
anxiolytic drug;
dermatologic drug;
H1-receptor antagonist
201720205.3low000030
ifenprodilpiperidines201720205.3low000030
1-(2-naphthalenyl)-3-[(phenylmethyl)-propan-2-ylamino]-1-propanonenaphthalenes201720205.3medium000030
ketaminecyclohexanones;
monochlorobenzenes;
secondary amino compound
analgesic;
environmental contaminant;
intravenous anaesthetic;
neurotoxin;
NMDA receptor antagonist;
xenobiotic
201720205.3low000030
ketoconazoledichlorobenzene;
dioxolane;
ether;
imidazoles;
N-acylpiperazine;
N-arylpiperazine
201820186.0low000010
ketoprofenbenzophenones;
oxo monocarboxylic acid
antipyretic;
drug allergen;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
environmental contaminant;
non-steroidal anti-inflammatory drug;
xenobiotic
201720205.3low000030
mebendazolearomatic ketone;
benzimidazoles;
carbamate ester
antinematodal drug;
microtubule-destabilising agent;
tubulin modulator
201720205.3low000030
mephenesinaromatic ether;
glycerol ether
201720205.3low000030
midazolamimidazobenzodiazepine;
monofluorobenzenes;
organochlorine compound
anticonvulsant;
antineoplastic agent;
anxiolytic drug;
apoptosis inducer;
central nervous system depressant;
GABAA receptor agonist;
general anaesthetic;
muscle relaxant;
sedative
201720177.0low000010
niclosamidebenzamides;
C-nitro compound;
monochlorobenzenes;
salicylanilides;
secondary carboxamide
anthelminthic drug;
anticoronaviral agent;
antiparasitic agent;
apoptosis inducer;
molluscicide;
piscicide;
STAT3 inhibitor
201720205.3low000030
oxibendazolebenzimidazoles;
carbamate ester
201720205.3low000030
4-(2'-methoxyphenyl)-1-(2'-(n-(2''-pyridinyl)-4-iodobenzamido)ethyl)piperazine201720205.3low000030
pentamidinearomatic ether;
carboxamidine;
diether
anti-inflammatory agent;
antifungal agent;
calmodulin antagonist;
chemokine receptor 5 antagonist;
EC 2.3.1.48 (histone acetyltransferase) inhibitor;
NMDA receptor antagonist;
S100 calcium-binding protein B inhibitor;
trypanocidal drug;
xenobiotic
2009200915.0low000100
perphenazineN-(2-hydroxyethyl)piperazine;
N-alkylpiperazine;
organochlorine compound;
phenothiazines
antiemetic;
dopaminergic antagonist;
phenothiazine antipsychotic drug
201720205.3low000030
pimobendanbenzimidazoles;
pyridazinone
cardiotonic drug;
EC 3.1.4.* (phosphoric diester hydrolase) inhibitor;
vasodilator agent
201720205.3low000030
ag 1879aromatic amine;
monochlorobenzenes;
pyrazolopyrimidine
beta-adrenergic antagonist;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor;
geroprotector
201720205.3low000030
primaquineaminoquinoline;
aromatic ether;
N-substituted diamine
antimalarial2013201311.0low000010
pyrimethamineaminopyrimidine;
monochlorobenzenes
antimalarial;
antiprotozoal drug;
EC 1.5.1.3 (dihydrofolate reductase) inhibitor
2013201311.0low000020
3-[(3,5-dibromo-4-hydroxyphenyl)methylidene]-5-iodo-1H-indol-2-oneindoles201720205.5medium000020
ro 31-8220imidothiocarbamic ester;
indoles;
maleimides
EC 2.7.11.13 (protein kinase C) inhibitor201720205.3low000030
ropiniroleindolones;
tertiary amine
antidyskinesia agent;
antiparkinson drug;
central nervous system drug;
dopamine agonist
201720205.3low000030
vorinostatdicarboxylic acid diamide;
hydroxamic acid
antineoplastic agent;
apoptosis inducer;
EC 3.5.1.98 (histone deacetylase) inhibitor
201720205.3low000030
sulfaphenazoleprimary amino compound;
pyrazoles;
substituted aniline;
sulfonamide antibiotic;
sulfonamide
antibacterial drug;
EC 1.14.13.181 (13-deoxydaunorubicin hydroxylase) inhibitor;
EC 1.14.13.67 (quinine 3-monooxygenase) inhibitor;
P450 inhibitor
201820186.0low000010
2-[4-(4-chloro-1,2-diphenylbut-1-enyl)phenoxy]-N,N-dimethylethanaminestilbenoid201720205.5high000020
trifluperidolaromatic ketone201720177.0low000010
3-(5'-hydroxymethyl-2'-furyl)-1-benzylindazolearomatic primary alcohol;
furans;
indazoles
antineoplastic agent;
apoptosis inducer;
platelet aggregation inhibitor;
soluble guanylate cyclase activator;
vasodilator agent
201720205.3low000030
zotepinedibenzothiepine;
tertiary amino compound
alpha-adrenergic drug;
second generation antipsychotic;
serotonergic drug
201720205.3low000030
methylene blueorganic chloride saltacid-base indicator;
antidepressant;
antimalarial;
antimicrobial agent;
antioxidant;
cardioprotective agent;
EC 1.4.3.4 (monoamine oxidase) inhibitor;
EC 3.1.1.8 (cholinesterase) inhibitor;
EC 4.6.1.2 (guanylate cyclase) inhibitor;
fluorochrome;
histological dye;
neuroprotective agent;
physical tracer
2013201311.0low000010
colchicinealkaloid;
colchicine
anti-inflammatory agent;
gout suppressant;
mutagen
201720205.3low000030
benziodaronearomatic ketone201720205.3low000030
methylene chloridechloromethanes;
volatile organic compound
carcinogenic agent;
polar aprotic solvent;
refrigerant
2009200915.0low000100
cyclizineN-alkylpiperazineantiemetic;
central nervous system depressant;
cholinergic antagonist;
H1-receptor antagonist;
local anaesthetic
201920195.0low000010
trehalosetrehaloseEscherichia coli metabolite;
geroprotector;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
201720205.3low000030
triclocarbandichlorobenzene;
monochlorobenzenes;
phenylureas
antimicrobial agent;
antiseptic drug;
disinfectant;
environmental contaminant;
xenobiotic
201720205.3low000030
4-tert-octylphenolalkylbenzene201720205.3low000030
cycloguaniltriazinesantifolate;
antiinfective agent;
antimalarial;
antiparasitic agent;
antiprotozoal drug;
EC 1.5.1.3 (dihydrofolate reductase) inhibitor
2013201311.0low000010
ethamivanmethoxybenzenes;
phenols
201720205.3low000030
methysergideergoline alkaloid201720205.3low000030
emetineisoquinoline alkaloid;
pyridoisoquinoline
antiamoebic agent;
anticoronaviral agent;
antiinfective agent;
antimalarial;
antineoplastic agent;
antiprotozoal drug;
antiviral agent;
autophagy inhibitor;
emetic;
expectorant;
plant metabolite;
protein synthesis inhibitor
201720205.3low000030
melarsoproltriazines2007200717.0low000100
podophyllotoxinfuronaphthodioxole;
lignan;
organic heterotetracyclic compound
antimitotic;
antineoplastic agent;
keratolytic drug;
microtubule-destabilising agent;
plant metabolite;
tubulin modulator
201720205.3low000030
erythromycincyclic ketone;
erythromycin
201620168.0low000010
etonitazene201720205.3low000030
clothiapinedibenzothiazepine201720205.3low000030
benperidolaromatic ketone201720205.3low000030
7-hydroxychlorpromazinephenothiazines201720205.3medium000030
sulfadoxinepyrimidines;
sulfonamide
antibacterial drug;
antimalarial
2013201311.0low000010
camptothecindelta-lactone;
pyranoindolizinoquinoline;
quinoline alkaloid;
tertiary alcohol
antineoplastic agent;
EC 5.99.1.2 (DNA topoisomerase) inhibitor;
genotoxin;
plant metabolite
201720205.3low000030
thenalidinedialkylarylamine;
tertiary amino compound
201720205.3medium000030
decoquinate2013201311.0low000010
bromocriptineindole alkaloidantidyskinesia agent;
antiparkinson drug;
dopamine agonist;
hormone antagonist
201720205.3low000030
benzonidazoleC-nitro compound;
imidazoles;
monocarboxylic acid amide
antiprotozoal drug2007200717.0low000100
dexchlorpheniraminechlorphenamine201720205.3low000030
dv 1006201720205.3medium000030
climbazolearomatic ether;
hemiaminal ether;
imidazoles;
ketone;
monochlorobenzenes
201720205.3low000030
mefloquine[2,8-bis(trifluoromethyl)quinolin-4-yl]-(2-piperidyl)methanolantimalarial201320179.8low000050
triadimenolaromatic ether;
conazole fungicide;
hemiaminal ether;
monochlorobenzenes;
secondary alcohol;
triazole fungicide
antifungal agrochemical;
EC 1.14.13.70 (sterol 14alpha-demethylase) inhibitor;
xenobiotic metabolite
201720205.3medium000030
amonafideisoquinolines201720205.3low000030
flupirtineaminopyridine201720205.3low000030
chaetochromin201720205.3medium000030
enoximonearomatic ketone201720205.3low000030
aripiprazolearomatic ether;
delta-lactam;
dichlorobenzene;
N-alkylpiperazine;
N-arylpiperazine;
quinolone
drug metabolite;
H1-receptor antagonist;
second generation antipsychotic;
serotonergic agonist
201720205.3low000030
aloxistatinepoxide;
ethyl ester;
L-leucine derivative;
monocarboxylic acid amide
anticoronaviral agent;
cathepsin B inhibitor
201920195.0low000010
indocate201720205.3medium000030
N(4)-acetylsulfathiazole1,3-thiazoles;
acetamides;
sulfonamide
marine xenobiotic metabolite201720205.3high000030
cyclizine hydrochloride201720205.5medium000020
2,3-trimethylene-4-quinazolonequinazolines201720205.3medium000030
artemisininorganic peroxide;
sesquiterpene lactone
antimalarial;
plant metabolite
201520159.0low000010
artemetherartemisinin derivative;
cyclic acetal;
organic peroxide;
semisynthetic derivative;
sesquiterpenoid
antimalarial2008201313.6low000320
1,3-dimethyluric acidoxopurinemetabolite201720205.3low000030
danofloxacinquinolines201720205.3low000030
nitrefazoleimidazoles201720205.3medium000030
methotrimeprazinephenothiazines;
tertiary amine
anticoronaviral agent;
cholinergic antagonist;
dopaminergic antagonist;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
non-narcotic analgesic;
phenothiazine antipsychotic drug;
serotonergic antagonist
201720205.3low000030
honokiolbiphenyls201720205.3low000030
9-methoxyellipticine201720205.3low000030
3-aminophenoxazonephenoxazine201720205.3low000030
3-deazaneplanocin201720205.3low000030
tryptanthrinealkaloid antibiotic;
organic heterotetracyclic compound;
organonitrogen heterocyclic compound
201720205.3low000030
atovaquonehydroxy-1,2-naphthoquinone2007201612.0low000120
2-chlorodiazepam201720205.3medium000030
Polycartine Bphenazines201720205.3high000030
aminoquinuride dihydrochloride201720205.3high000030
thioproperazine mesylatephenothiazines201720205.3medium000030
n(6)-(delta(2)-isopentenyl)adenine6-isopentenylaminopurinecytokinin201720205.3low000030
4-methyl-N-(phenylmethyl)benzenesulfonamidesulfonamide201720205.3medium000030
zpck201920204.5low000020
sr141716amidopiperidine;
carbohydrazide;
dichlorobenzene;
monochlorobenzenes;
pyrazoles
anti-obesity agent;
appetite depressant;
CB1 receptor antagonist
201720205.3low000030
(6R)-7-[4-(dimethylamino)phenyl]-N-hydroxy-4,6-dimethyl-7-oxohepta-2,4-dienamidearomatic ketone201720205.5high000020
pyronaridineaminoquinoline2013201311.0low000010
fingolimodaminodiol;
primary amino compound
antineoplastic agent;
CB1 receptor antagonist;
immunosuppressive agent;
prodrug;
sphingosine-1-phosphate receptor agonist
201720205.3low000030
tesmilifenediarylmethane201720205.3low000030
tafenoquine(trifluoromethyl)benzenes;
aminoquinoline;
aromatic ether;
primary amino compound;
secondary amino compound
2013201311.0low000010
sr 27897indolyl carboxylic acid201720205.3low000030
piperaquineaminoquinoline;
N-arylpiperazine;
organochlorine compound
antimalarial2013201311.0low000020
n-(n-(3-carboxyoxirane-2-carbonyl)leucyl)isoamylamineleucine derivative201720205.3low000030
norketamineorganochlorine compound201720205.3low000030
indatralineindanes201920204.5low000020
methotrexatedicarboxylic 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
201720205.3low000030
salvinorin aorganic heterotricyclic compound;
organooxygen compound
metabolite;
oneirogen
201920195.0low000010
4-diethoxyphosphorylmethyl-n-(4-bromo-2-cyanophenyl)benzamide201720205.3low000030
n,n-di-n-hexyl-2-(4-fluorophenyl)indole-3-acetamidephenylindole201720205.3low000030
l 741626piperidines201720205.3low000030
tempolaminoxyls;
hydroxypiperidine
anti-inflammatory agent;
antineoplastic agent;
apoptosis inducer;
catalyst;
hepatoprotective agent;
nephroprotective agent;
neuroprotective agent;
radical scavenger
2010201014.0low000100
dx 8951pyranoindolizinoquinoline201720205.3low000030
tipifarnibimidazoles;
monochlorobenzenes;
primary amino compound;
quinolone
antineoplastic agent;
apoptosis inducer;
EC 2.5.1.58 (protein farnesyltransferase) inhibitor
201720205.3low000030
cyc 2022,6-diaminopurinesantiviral drug;
EC 2.7.11.22 (cyclin-dependent kinase) inhibitor
201720205.3low000030
3-(n-acetyl-n-hydroxy)aminopropylphosphonic acidphosphonoacetic acid201620168.0low000010
avasimibemonoterpenoid201720205.3low000030
speciophyllineindolizines202220222.0medium000001
erysodinearomatic ether;
diether;
Erythrina alkaloid;
organic heterotetracyclic compound;
phenols
antiparasitic agent;
nicotinic antagonist;
phytogenic insecticide
202220222.0low000001
l 163191201720205.3low000030
dizocilpinesecondary amino compound;
tetracyclic antidepressant
anaesthetic;
anticonvulsant;
neuroprotective agent;
nicotinic antagonist;
NMDA receptor antagonist
201720205.3low000030
s-benzylcysteineS-aryl-L-cysteine zwitterion201720205.3high000030
chelidoninealkaloid antibiotic;
alkaloid fundamental parent;
benzophenanthridine alkaloid
201720205.3low000030
lapatinibfurans;
organochlorine compound;
organofluorine compound;
quinazolines
antineoplastic agent;
tyrosine kinase inhibitor
201720205.3low000030
roxindoleindolesalpha-adrenergic antagonist;
serotonergic drug
201720205.3low000030
conidendrin201720205.3high000030
Porfiromycinemitomycin201720205.3high000030
nsc 953971,4-naphthoquinones201720205.3low000030
4-methyl-2-quinazolinamine201720205.3high000030
2-glycineamide-5-chlorophenyl-2-pyrryl ketone201720205.3high000030
niguldipine hydrochloride201920204.5medium000020
2,5-bis(5-hydroxymethyl-2-thienyl)furanthiophenes201720205.3low000030
ritonavir1,3-thiazoles;
carbamate ester;
carboxamide;
L-valine derivative;
ureas
antiviral drug;
environmental contaminant;
HIV protease inhibitor;
xenobiotic
201720205.3low000030
bardoxolone methylcyclohexenones201920195.0low000010
Destruxin Bcyclodepsipeptide201720205.3high000030
tosylphenylalanyl chloromethyl ketonealpha-chloroketone;
sulfonamide
alkylating agent;
serine proteinase inhibitor
201720205.3low000030
quinidinecinchona alkaloidalpha-adrenergic antagonist;
anti-arrhythmia drug;
antimalarial;
drug allergen;
EC 1.14.13.181 (13-deoxydaunorubicin hydroxylase) inhibitor;
EC 3.6.3.44 (xenobiotic-transporting ATPase) inhibitor;
muscarinic antagonist;
P450 inhibitor;
potassium channel blocker;
sodium channel blocker
201820186.0low000010
mefloquine hydrochloride2009200915.0low000100
trichostatin aantibiotic antifungal agent;
hydroxamic acid;
trichostatin
bacterial metabolite;
EC 3.5.1.98 (histone deacetylase) inhibitor;
geroprotector
201920195.0low000010
thapsigarginbutyrate ester;
organic heterotricyclic compound;
sesquiterpene lactone
calcium channel blocker;
EC 3.6.3.8 (Ca(2+)-transporting ATPase) inhibitor
2007200717.0low000100
clindamycin201620168.0low000010
zithromaxmacrolide antibioticantibacterial drug;
environmental contaminant;
xenobiotic
201620168.0low000010
artenimol201720224.0low000012
sitafloxacinfluoroquinolone antibiotic;
quinolines;
quinolone antibiotic
201920195.0low000010
2'-c-methylcytidine201720205.3low000030
triacetoneamine-n-oxylaminoxyls;
piperidones
radical scavenger2010201014.0low000100
jp-1302201720205.3medium000030
7-chloro-5,10-dihydrothieno[3,4-b][1,5]benzodiazepin-4-onebenzodiazepine201720205.3high000030
tenatoprazoleimidazopyridine201720205.3low000030
s 1033(trifluoromethyl)benzenes;
imidazoles;
pyridines;
pyrimidines;
secondary amino compound;
secondary carboxamide
anticoronaviral agent;
antineoplastic agent;
tyrosine kinase inhibitor
201720205.3low000030
5-[(2-fluoroanilino)methyl]-8-quinolinolhydroxyquinoline201720205.3high000030
benidipine hydrochloride201720205.5low000020
benidipine201920195.0low000010
2-(1,3-benzoxazol-2-ylamino)-5-spiro[1,6,7,8-tetrahydroquinazoline-4,1'-cyclopentane]onequinazolines201720205.3high000030
chlorprothixenechlorprothixene201720205.3medium000030
jrf 12201720205.3low000030
5-amino-3-(4-methoxyphenyl)-4-oxo-1-thieno[3,4-d]pyridazinecarboxylic acid ethyl estermethoxybenzenes;
substituted aniline
201720205.3high000030
3-hydroxypyridine, sodium salt201720205.3high000030
N-(3-cyano-4,5,6,7-tetrahydro-1-benzothiophen-2-yl)-1-naphthalenecarboxamidenaphthalenecarboxamide201720205.3medium000030
5-[(2-bromoanilino)methyl]-8-quinolinolhydroxyquinoline201720205.3high000030
3-amino-n-(4-methoxybenzyl)-4,6-dimethylthieno(2,3-b)pyridine-2-carboxamide201720205.3medium000030
N-[(2-methoxyphenyl)methyl]-4-(1-piperidinyl)anilinearomatic amine201720205.3high000030
1-[4-(4-bromophenyl)-2-thiazolyl]-4-piperidinecarboxamidepiperidinecarboxamide201720205.3high000030
5-[[2-(trifluoromethyl)anilino]methyl]-8-quinolinolhydroxyquinoline201720205.3high000030
N-[3-[2-[(4-methyl-2-pyridinyl)amino]-4-thiazolyl]phenyl]acetamideacetamides;
anilide
201720205.3high000030
5-bromo-N-(5-cyclohexyl-1,3,4-thiadiazol-2-yl)-2-thiophenecarboxamidearomatic amide;
thiophenes
201720205.3high000030
6-amino-1-[2-(3,4-dimethoxyphenyl)ethyl]-2-sulfanylidene-4-pyrimidinonedimethoxybenzene201720205.3high000030
N-[4-[(3,4-dimethyl-5-isoxazolyl)sulfamoyl]phenyl]-6,8-dimethyl-2-(2-pyridinyl)-4-quinolinecarboxamidearomatic amide201720205.3high000030
N-[5-[(4-chlorophenoxy)methyl]-1,3,4-thiadiazol-2-yl]-5-methyl-3-phenyl-4-isoxazolecarboxamidearomatic ether201720205.3high000030
3-chloro-1-(2,5-dimethoxyphenyl)-4-(1-piperidinyl)pyrrole-2,5-dionemaleimides201720205.3high000030
Src Inhibitor-1aromatic ether;
polyether;
quinazolines;
secondary amino compound
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor201720205.3high000030
1-[2-(3,4-dimethoxyphenyl)ethyl]-6-propyl-2-sulfanylidene-7,8-dihydro-5H-pyrimido[4,5-d]pyrimidin-4-onedimethoxybenzene201720205.3high000030
2-phenyl-N-[4-(2-thiazolylsulfamoyl)phenyl]-4-quinolinecarboxamidequinolines201720205.3high000030
3-(2,5-dimethyl-1-phenyl-3-pyrrolyl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepinepyrroles201720205.3high000030
tempoaminoxyls;
piperidines
catalyst;
ferroptosis inhibitor;
radical scavenger
2010201014.0low000100
bi-78d3aryl sulfide201720205.3medium000030
kartogenin201720205.3low000030
toremifenearomatic ether;
organochlorine compound;
tertiary amine
antineoplastic agent;
bone density conservation agent;
estrogen antagonist;
estrogen receptor modulator
201920195.0low000010
quininecinchona alkaloidantimalarial;
muscle relaxant;
non-narcotic analgesic
2013201311.0low000010
vx-745aryl sulfide;
dichlorobenzene;
difluorobenzene;
pyrimidopyridazine
anti-inflammatory drug;
apoptosis inducer;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor
201720205.3low000030
dasatinib1,3-thiazoles;
aminopyrimidine;
monocarboxylic acid amide;
N-(2-hydroxyethyl)piperazine;
N-arylpiperazine;
organochlorine compound;
secondary amino compound;
tertiary amino compound
anticoronaviral agent;
antineoplastic agent;
tyrosine kinase inhibitor
201720205.3low000030
tempo carboxylic acidaminoxyls;
piperidinemonocarboxylic acid
MRI contrast agent;
radical scavenger;
spin label
2010201014.0medium000100
zd 6474aromatic ether;
organobromine compound;
organofluorine compound;
piperidines;
quinazolines;
secondary amine
antineoplastic agent;
tyrosine kinase inhibitor
201720205.3low000030
N-[2-(diethylamino)ethyl]-5-[(5-fluoro-2-oxo-1H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamideindoles201920204.5high000020
nih-12848201720205.3high000030
2,4-dioxo-3-pentyl-N-[3-(1-piperidinyl)propyl]-1H-quinazoline-7-carboxamidequinazolines201720205.3high000030
[1-(3-methylphenyl)-5-benzimidazolyl]-(1-piperidinyl)methanonebenzimidazoles201720205.3high000030
2-[[(6-bromo-1H-imidazo[4,5-b]pyridin-2-yl)thio]methyl]benzonitrileimidazopyridine201720205.3high000030
3-[(3-fluorophenyl)methyl]-8-[4-(4-fluorophenyl)-4-oxobutyl]-1-phenyl-1,3,8-triazaspiro[4.5]decan-4-onearomatic ketone201720205.3high000030
4-[[7-[(4-fluorophenyl)methyl]-1,3-dimethyl-2,6-dioxo-8-purinyl]methyl]-1-piperazinecarboxylic acid ethyl esteroxopurine201720205.3high000030
N,N-dimethylcarbamodithioic acid (1-acetamido-2,2,2-trichloroethyl) esterorganonitrogen compound;
organosulfur compound
201720205.3high000030
6-bromo-2-(4-methylphenyl)-N-[(1-methyl-4-pyrazolyl)methyl]-4-quinolinecarboxamidequinolines201720205.3high000030
LSM-1924organic heterotricyclic compound;
organooxygen compound
201720205.3high000030
ferrostatin-1ethyl ester;
primary arylamine;
substituted aniline
antifungal agent;
antioxidant;
ferroptosis inhibitor;
neuroprotective agent;
radiation protective agent;
radical scavenger
201720205.3low000030
6-(2-methyl-1-piperidinyl)-5-nitro-4-pyrimidinamineC-nitro compound201720205.3high000030
rabeprazole(1-)organic nitrogen anion201920204.5high000020
ncgc00099374201720205.3high000030
2-nitro-4-[(6-nitro-4-quinolinyl)amino]-N-[4-(pyridin-4-ylamino)phenyl]benzamidebenzamides201720205.3high000030
luteolin3'-hydroxyflavonoid;
tetrahydroxyflavone
angiogenesis inhibitor;
anti-inflammatory agent;
antineoplastic agent;
apoptosis inducer;
c-Jun N-terminal kinase inhibitor;
EC 2.3.1.85 (fatty acid synthase) inhibitor;
immunomodulator;
nephroprotective agent;
plant metabolite;
radical scavenger;
vascular endothelial growth factor receptor antagonist
201720205.3low000030
cyclosporine201920195.0low000010
kaempferol7-hydroxyflavonol;
flavonols;
tetrahydroxyflavone
antibacterial agent;
geroprotector;
human blood serum metabolite;
human urinary metabolite;
human xenobiotic metabolite;
plant metabolite
201720205.3low000030
genistein7-hydroxyisoflavonesantineoplastic agent;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor;
geroprotector;
human urinary metabolite;
phytoestrogen;
plant metabolite;
tyrosine kinase inhibitor
201720205.3low000030
mycophenolate mofetilcarboxylic ester;
ether;
gamma-lactone;
phenols;
tertiary amino compound
anticoronaviral agent;
EC 1.1.1.205 (IMP dehydrogenase) inhibitor;
immunosuppressive agent;
prodrug
201720205.3medium000030
bruceantintriterpenoid201720205.3low000030
chrysin7-hydroxyflavonol;
dihydroxyflavone
anti-inflammatory agent;
antineoplastic agent;
antioxidant;
EC 2.7.11.18 (myosin-light-chain kinase) inhibitor;
hepatoprotective agent;
plant metabolite
201720205.3low000030
daidzein7-hydroxyisoflavonesantineoplastic agent;
EC 2.7.7.7 (DNA-directed DNA polymerase) inhibitor;
EC 3.2.1.20 (alpha-glucosidase) inhibitor;
phytoestrogen;
plant metabolite
201720205.3low000030
neticonazolearomatic ether;
benzenes;
conazole antifungal drug;
enamine;
imidazole antifungal drug;
imidazoles;
methyl sulfide
antifungal drug;
EC 1.14.13.70 (sterol 14alpha-demethylase) inhibitor
201720205.3medium000030
N-(4Z,7Z,10Z,13Z,16Z,19Z)-docosahexaenoylethanolamineendocannabinoid;
N-acylethanolamine 22:6
201720205.3medium000030
n-oleoylethanolamineendocannabinoid;
N-(long-chain-acyl)ethanolamine;
N-acylethanolamine 18:1
EC 3.5.1.23 (ceramidase) inhibitor;
geroprotector;
PPARalpha agonist
201720205.3low000030
alpha-zearalenolmacrolide201720205.3high000030
su 9516201720205.3low000030
N-(4-bromo-3-methylphenyl)-2,5-dimethyl-[1,2,4]triazolo[1,5-a]pyrimidin-7-aminetriazolopyrimidines201720205.3high000030
sb 277011201720205.3low000030
sb 223412201720205.3low000030
sr 59230atetralins201720205.3high000030
3-[6-[4-(trifluoromethoxy)anilino]-4-pyrimidinyl]benzamidepyrimidines201720205.3medium000030
kn 62piperazines201720205.3low000030
erysovine202220222.0medium000001
erythralinealkaloid202220222.0medium000001
MeJAJasmonate derivatives201720205.3high000030
1h-pyrrole-2,5-dione, 3-(1-methyl-1h-indol-3-yl)-4-(1-methyl-6-nitro-1h-indol-3-yl)-201720205.3high000030
pd 161570201720205.3medium000030
su 11248monocarboxylic acid amide;
pyrroles
angiogenesis inhibitor;
antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
immunomodulator;
neuroprotective agent;
vascular endothelial growth factor receptor antagonist
201720177.0low000010
palbociclibaminopyridine;
aromatic ketone;
cyclopentanes;
piperidines;
pyridopyrimidine;
secondary amino compound;
tertiary amino compound
antineoplastic agent;
EC 2.7.11.22 (cyclin-dependent kinase) inhibitor
201720205.3low000030
jnj-7706621sulfonamide201720205.3low000030
virginiamycin factor s1cyclodepsipeptide;
macrolide antibiotic
antibacterial drug;
bacterial metabolite
201720205.3high000030
fenoterolhydrobromidebeta-adrenergic agonist;
bronchodilator agent;
sympathomimetic agent
201920204.5low000020
xib 4035201720205.3high000030
gw-5074201920195.0low000010
proguanilbiguanides;
monochlorobenzenes
antimalarial;
antiprotozoal drug;
EC 1.5.1.3 (dihydrofolate reductase) inhibitor
2013201311.0low000010
psammaplin a2009200915.0low000100
lumefantrinefluorenes;
monochlorobenzenes;
secondary alcohol;
tertiary amine
antimalarial2013201311.0low000010
belotecanpyranoindolizinoquinoline201720205.3low000030
norgestimateketoxime;
steroid ester;
terminal acetylenic compound
contraceptive drug;
progestin;
synthetic oral contraceptive
201720205.3high000030
b 43aromatic amine;
aromatic ether;
cyclopentanes;
primary amino compound;
pyrrolopyrimidine
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor;
geroprotector
201720205.3medium000030
4-(2' methoxyphenyl)-1-(2'-(n-(2''-pyridinyl)-4-fluorobenzamido)ethyl)piperazine201720205.3medium000030
methiazolebenzimidazoles;
carbamate ester
201720205.3high000030
sb 218795quinolines201720205.3medium000030
bvt.948201720205.3high000030
fk 866benzamides;
N-acylpiperidine
201920195.0low000010
a 38503201720205.3medium000030
artesunateartemisinin derivative;
cyclic acetal;
dicarboxylic acid monoester;
hemisuccinate;
semisynthetic derivative;
sesquiterpenoid
antimalarial;
antineoplastic agent;
ferroptosis inducer
2007201812.0low000240
parthenolidesesquiterpene lactonedrug allergen;
inhibitor;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
peripheral nervous system drug
201720196.0medium000020
krn 633201720205.3medium000030
5-amino-4-oxo-3-phenyl-1-thieno[3,4-d]pyridazinecarboxylic acidorganonitrogen heterocyclic compound;
organosulfur heterocyclic compound
201720205.3high000030
gw 5015161,3-thiazoles;
aromatic ether;
aryl sulfide;
monocarboxylic acid;
organofluorine compound
carcinogenic agent;
PPARbeta/delta agonist
201720205.3low000030
dolastatin 101,3-thiazoles;
tetrapeptide
animal metabolite;
antineoplastic agent;
apoptosis inducer;
marine metabolite;
microtubule-destabilising agent
201720205.3low000030
spc-839201720205.3low000030
midostaurinbenzamides;
gamma-lactam;
indolocarbazole;
organic heterooctacyclic compound
antineoplastic agent;
EC 2.7.11.13 (protein kinase C) inhibitor
201720205.3low000030
valnemulin201920204.5medium000020
nu 7026organic heterotricyclic compound;
organooxygen compound
201720205.3low000030
osi 930aromatic amide201720205.3medium000030
ticagreloraryl sulfide;
hydroxyether;
organofluorine compound;
secondary amino compound;
triazolopyrimidines
P2Y12 receptor antagonist;
platelet aggregation inhibitor
201720205.3low000030
l 692585peptide201720205.3high000030
pi103aromatic amine;
morpholines;
organic heterotricyclic compound;
phenols;
tertiary amino compound
antineoplastic agent;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor;
mTOR inhibitor
201720205.3low000030
mer nf5003f202220222.0medium000001
nnc 26-9100aminopyridine201720205.3medium000030
2-(3-chlorobenzyloxy)-6-(piperazin-1-yl)pyrazine201720205.3high000030
tivozanibaromatic ether201720205.3low000030
hki 272nitrile;
quinolines
antineoplastic agent;
tyrosine kinase inhibitor
201920195.0low000010
1,2,6,7-tetraoxaspiro(7.11)nonadecane202220222.0low000001
n-(6-chloro-7-methoxy-9h-beta-carbolin-8-yl)-2-methylnicotinamide201720205.3medium000030
tae226morpholines201720205.3low000030
gw0742monocarboxylic acid201720205.3low000030
u 18666ahydrochlorideantiviral agent;
EC 1.3.1.72 (Delta(24)-sterol reductase) inhibitor;
Hedgehog signaling pathway inhibitor;
nicotinic antagonist;
sterol biosynthesis inhibitor
201720205.3low000030
sb 525334quinoxaline derivative201720205.3low000030
bx795ureas201720205.3low000030
azd 6244benzimidazoles;
bromobenzenes;
hydroxamic acid ester;
monochlorobenzenes;
organofluorine compound;
secondary amino compound
anticoronaviral agent;
antineoplastic agent;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor
201720205.3low000030
1-(2-(1-adamantyl)ethyl)-1-pentyl-3-(3-(4-pyridyl)propyl)urea201720205.3medium000030
bay 61-3606pyrimidines201720205.3medium000030
artenimol2008201313.2low000220
sd-208201720205.3low000030
crenolanibaminopiperidine;
aromatic ether;
benzimidazoles;
oxetanes;
quinolines;
tertiary amino compound
angiogenesis inhibitor;
antineoplastic agent;
apoptosis inducer;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor
201720205.3low000030
aculeatin a202220222.0medium000001
cj 033466201720205.3high000030
cc 401pyrazoles;
ring assembly
201720205.3medium000030
PB28aromatic ether;
piperazines;
tetralins
anticoronaviral agent;
antineoplastic agent;
apoptosis inducer;
sigma-2 receptor agonist
201720205.3low000030
cariprazine201720205.3low000030
krp-203201720205.3high000030
regorafenib(trifluoromethyl)benzenes;
aromatic ether;
monochlorobenzenes;
monofluorobenzenes;
phenylureas;
pyridinecarboxamide
antineoplastic agent;
hepatotoxic agent;
tyrosine kinase inhibitor
201720205.3low000030
at 7867monochlorobenzenes;
piperidines;
pyrazoles
antineoplastic agent;
EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor
201720205.3high000030
acetic acid 2-[4-methyl-8-(4-morpholinylsulfonyl)-1,3-dioxo-2-pyrrolo[3,4-c]quinolinyl]ethyl esterpyrroloquinoline201720205.3high000030
ptc 124oxadiazole;
ring assembly
201720205.3low000030
degrasyn201920204.5low000020
marizomibbeta-lactone;
gamma-lactam;
organic heterobicyclic compound;
organochlorine compound;
salinosporamide
antineoplastic agent;
proteasome inhibitor
2013201311.0low000010
bi 2536201720205.3low000030
azd 1152anilide;
monoalkyl phosphate;
monofluorobenzenes;
pyrazoles;
quinazolines;
secondary amino compound;
secondary carboxamide;
tertiary amino compound
antineoplastic agent;
Aurora kinase inhibitor;
prodrug
201720205.3medium000030
artemisone2013201311.0low000010
carfilzomibepoxide;
morpholines;
tetrapeptide
antineoplastic agent;
proteasome inhibitor
201720205.3low000030
idelalisibaromatic amine;
organofluorine compound;
purines;
quinazolines;
secondary amino compound
antineoplastic agent;
apoptosis inducer;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor
201720205.3low000030
motesanibpyridinecarboxamide201720205.3medium000030
pf-562,271indoles201720205.3medium000030
gliocladin c201720205.3high000030
sb 706504201720205.3high000030
ku-0060648dibenzothiophenes201720205.3medium000030
bgt226aromatic ether;
imidazoquinoline;
N-arylpiperazine;
organofluorine compound;
pyridines
antineoplastic agent;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor;
mTOR inhibitor
201720205.3medium000030
deoxyartemisinin2007201015.5high000200
cladosporin2013201311.0low000010
n-desmethyldanofloxacin201720205.3high000030
rabeprazole sodiumorganic sodium salt201720177.0low000010
azd 1152-hqpaanilide;
monofluorobenzenes;
primary alcohol;
pyrazoles;
quinazolines;
secondary amino compound;
secondary carboxamide;
tertiary amino compound
antineoplastic agent;
Aurora kinase inhibitor
201920204.5low000020
CDN1163aromatic ether;
quinolines;
secondary carboxamide
SERCA activator201720205.3medium000030
amodiaquine hydrochloride2013201311.0low000020
gsk 269962a201720205.3medium000030
pha 848125201720205.3medium000030
nvp-bhg712benzamides201720205.3medium000030
pf 04217903quinolines201720205.3medium000030
5-[[4-(4-acetylphenyl)-1-piperazinyl]sulfonyl]-1,3-dihydroindol-2-onearomatic ketone201720205.3high000030
ph 797804aromatic ether;
benzamides;
organobromine compound;
organofluorine compound;
pyridone
anti-inflammatory agent;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor
201720205.3low000030
srt1720201720205.3low000030
purfalcamine201720205.3high000030
bms 754807pyrazoles;
pyridines;
pyrrolidines;
pyrrolotriazine
antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor
201720205.3low000030
ponatinib(trifluoromethyl)benzenes;
acetylenic compound;
benzamides;
imidazopyridazine;
N-methylpiperazine
antineoplastic agent;
tyrosine kinase inhibitor
201720205.3low000030
quizartinibbenzoimidazothiazole;
isoxazoles;
morpholines;
phenylureas
antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
necroptosis inhibitor
201720205.3low000030
PP121aromatic amine;
cyclopentanes;
pyrazolopyrimidine;
pyrrolopyridine
antineoplastic agent;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor;
tyrosine kinase inhibitor
201720205.3medium000030
navitoclaxaryl sulfide;
monochlorobenzenes;
morpholines;
N-sulfonylcarboxamide;
organofluorine compound;
piperazines;
secondary amino compound;
sulfone;
tertiary amino compound
antineoplastic agent;
apoptosis inducer;
B-cell lymphoma 2 inhibitor
201720205.3low000030
oz 439201120227.9high000082
gsk 650394phenylpyridine201720205.3medium000030
dcc-2036organofluorine compound;
phenylureas;
pyrazoles;
pyridinecarboxamide;
quinolines
tyrosine kinase inhibitor201720205.3medium000030
cabozantinibaromatic ether;
dicarboxylic acid diamide;
organofluorine compound;
quinolines
antineoplastic agent;
tyrosine kinase inhibitor
201720205.3low000030
bix 01294piperidines2013201311.0low000010
TAK-5801,3-thiazolecarboxamide;
aminopyrimidine;
chloropyridine;
organofluorine compound;
pyrimidinecarboxamide;
secondary carboxamide
antineoplastic agent;
apoptosis inducer;
B-Raf inhibitor
201720205.3medium000030
8-(4-aminophenyl)-2-(4-morpholinyl)-1-benzopyran-4-onechromones201720205.3high000030
pf 3758309organic heterobicyclic compound;
organonitrogen heterocyclic compound;
organosulfur heterocyclic compound
201720205.3low000030
(5-(2,4-bis((3s)-3-methylmorpholin-4-yl)pyrido(2,3-d)pyrimidin-7-yl)-2-methoxyphenyl)methanolbenzyl alcohols;
morpholines;
pyridopyrimidine;
tertiary amino compound
antineoplastic agent;
apoptosis inducer;
mTOR inhibitor
201920204.5low000020
5-(2-benzofuranyl)-4-[(1-methyl-5-tetrazolyl)thio]thieno[2,3-d]pyrimidinearyl sulfide;
thienopyrimidine
201720205.3high000030
5-(3-methylsulfonylphenyl)-4-[(1-methyl-5-tetrazolyl)thio]thieno[2,3-d]pyrimidinearyl sulfide;
thienopyrimidine
201720205.3high000030
5-bromo-4-[(1-methyl-5-tetrazolyl)thio]thieno[2,3-d]pyrimidinearyl sulfide;
thienopyrimidine
201720205.3high000030
baricitinibazetidines;
nitrile;
pyrazoles;
pyrrolopyrimidine;
sulfonamide
anti-inflammatory agent;
antirheumatic drug;
antiviral agent;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor;
immunosuppressive agent
201720205.3low000030
6-(1,3-benzodioxol-5-yl)-N-methyl-N-(thiophen-2-ylmethyl)-4-quinazolinaminequinazolines201720205.3high000030
6-[(3-aminophenyl)methyl]-4-methyl-2-methylsulfinyl-5-thieno[3,4]pyrrolo[1,3-d]pyridazinoneorganic heterobicyclic compound;
organonitrogen heterocyclic compound;
organosulfur heterocyclic compound
201720205.3medium000030
sodium artesunate2009200915.0low000100
N-[(5-bromo-8-hydroxy-7-quinolinyl)-thiophen-2-ylmethyl]acetamidehydroxyquinoline201720205.3high000030
p505-15201720205.3high000030
mrt67307aromatic amine201720205.3medium000030
nitd 6092013201311.0low000020
N-[3-[[5-chloro-2-[4-(4-methyl-1-piperazinyl)anilino]-4-pyrimidinyl]oxy]phenyl]-2-propenamidepiperazines201720205.3high000030
ribociclib201720205.3low000030
1-[3-[4-[(1-methyl-5-tetrazolyl)thio]-5-thieno[2,3-d]pyrimidinyl]phenyl]ethanonearomatic ketone;
thienopyrimidine
201720205.3high000030
pha 793887piperidinecarboxamide201720205.3high000030
gsk 2334470indazoles201920195.0low000010
rka 182201320226.3high000021
ml228 probe1,2,4-triazines;
biphenyls;
pyridines;
secondary amino compound
hypoxia-inducible factor pathway activator201720205.3high000030
pf-03882845201720205.3high000030
jq1 compoundcarboxylic ester;
organochlorine compound;
tert-butyl ester;
thienotriazolodiazepine
angiogenesis inhibitor;
anti-inflammatory agent;
antineoplastic agent;
apoptosis inducer;
bromodomain-containing protein 4 inhibitor;
cardioprotective agent;
ferroptosis inducer
201720205.3low000030
pf-04620110201720205.3medium000030
gsk525762abenzodiazepine201720205.3low000030
birinapantdipeptide201920195.0low000010
torin 1N-acylpiperazine;
N-arylpiperazine;
organofluorine compound;
pyridoquinoline;
quinolines
antineoplastic agent;
mTOR inhibitor
201720205.3medium000030
abt-199aromatic ether;
C-nitro compound;
monochlorobenzenes;
N-alkylpiperazine;
N-arylpiperazine;
N-sulfonylcarboxamide;
oxanes;
pyrrolopyridine
antineoplastic agent;
apoptosis inducer;
B-cell lymphoma 2 inhibitor
201720205.3low000030
1-[4-fluoro-3-(trifluoromethyl)phenyl]-3-(5-pyridin-4-yl-1,3,4-thiadiazol-2-yl)ureaureas201720205.3medium000030
N-(4-methyl-2-pyridinyl)-4-[3-(trifluoromethyl)anilino]-1-piperidinecarbothioamide(trifluoromethyl)benzenes201720205.3high000030
ncgc00242364quinazolines201720205.3high000030
gsk1210151aimidazoquinoline201720205.3low000030
hs-173201720205.3high000030
sr1664indolecarboxamide201720205.3high000030
4-(3-chloro-5-(trifluoromethyl)pyridin-2-yl)-n-(4-methoxypyridin-2-yl)piperazine-1-carbothioamide201720205.3high000030
N-[4-(1-benzoyl-4-piperidinyl)butyl]-3-(3-pyridinyl)-2-propenamidebenzamides;
N-acylpiperidine
201720205.5high000020
N-[4-[3-chloro-4-(2-pyridinylmethoxy)anilino]-3-cyano-7-ethoxy-6-quinolinyl]-4-(dimethylamino)-2-butenamideaminoquinoline201720205.5high000020
cudc-907201720205.3low000030
methacycline201920195.0low000010
methacycline monohydrochloride201720205.5low000020
2-[[[4-hydroxy-2-oxo-1-(phenylmethyl)-3-quinolinyl]-oxomethyl]amino]acetic acidquinolines201720205.3high000030
agi-5198201720205.3low000030
cep-32496201720205.3medium000030
epz004777N-glycosyl compound201720205.3low000030
3-[[2-(2-pyridinyl)-6-(1,2,4,5-tetrahydro-3-benzazepin-3-yl)-4-pyrimidinyl]amino]propanoic acidorganonitrogen heterocyclic compound201720205.3medium000030
entecavirbenzamides;
N-acylpiperidine
201720205.3medium000030
gkt137831201720205.3low000030
vx-509201720205.3high000030
vx-970sulfonamide201720205.3low000030
gs-9973201720205.3high000030
amg 925201720205.3high000030
gne-618201720205.3high000030
6-chloro-7-methoxy-2-methyl-3-(4-(4-(trifluoromethoxy)phenoxy)phenyl)quinolin-4(1h)-one201620168.0low000010
g007-lk201720205.3medium000030
volitinib201720205.3high000030
ML355benzothiazoles;
monomethoxybenzene;
phenols;
secondary amino compound;
substituted aniline;
sulfonamide
EC 1.13.11.31 (arachidonate 12-lipoxygenase) inhibitor;
platelet aggregation inhibitor
201720205.3high000030
acp-196aromatic amine;
benzamides;
imidazopyrazine;
pyridines;
pyrrolidinecarboxamide;
secondary carboxamide;
tertiary carboxamide;
ynone
antineoplastic agent;
apoptosis inducer;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor
201720205.3low000030
gsk343aminopyridine;
indazoles;
N-alkylpiperazine;
N-arylpiperazine;
pyridone;
secondary carboxamide
antineoplastic agent;
apoptosis inducer;
EC 2.1.1.43 (enhancer of zeste homolog 2) inhibitor
201720205.3low000030
agi-6780201720205.3medium000030
khs101201720205.3medium000030
cb-839201720205.3low000030
gsk-j4organonitrogen heterocyclic compound201720205.3low000030
pf-06424439201720205.3high000030
etp-46464201720205.3high000030
onc201201720205.3low000030
kai407201720205.3high000030
6,7-dimethoxy-2-(pyrrolidin-1-yl)-n-(5-(pyrrolidin-1-yl)pentyl)quinazolin-4-amine201720205.3high000030
enasidenib1,3,5-triazines;
aminopyridine;
aromatic amine;
organofluorine compound;
secondary amino compound;
tertiary alcohol
antineoplastic agent;
EC 1.1.1.42 (isocitrate dehydrogenase) inhibitor
201720205.3low000030
oicr-9429201720205.3medium000030
lly-507201720205.3medium000030
at 9283201720205.3medium000030
hypoxanthinenucleobase analogue;
oxopurine;
purine nucleobase
fundamental metabolite201720205.3low000030
clozapinebenzodiazepine;
N-arylpiperazine;
N-methylpiperazine;
organochlorine compound
adrenergic antagonist;
dopaminergic antagonist;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
environmental contaminant;
GABA antagonist;
histamine antagonist;
muscarinic antagonist;
second generation antipsychotic;
serotonergic antagonist;
xenobiotic
201720205.3low000030
1-hydroxyphenazinephenazines201720205.3low000030
ro 24-7429benzodiazepine201720205.3medium000030
nintedanib201720205.3low000030
n'-(3,4-dihydroxybenzylidene)-3-hydroxy-2-naphthahydrazidecatechols;
hydrazide;
hydrazone;
naphthols
EC 3.6.5.5 (dynamin GTPase) inhibitor201720205.3high000030
ver 52296aromatic amide;
isoxazoles;
monocarboxylic acid amide;
morpholines;
resorcinols
angiogenesis inhibitor;
antineoplastic agent;
Hsp90 inhibitor
201720205.3low000030
rvx 208201720205.3low000030
bmn 673201720205.3low000030
SubstanceStudiesClassesRolesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
carbamatesamino-acid anion2011201113.0low000010
amodiaquineaminoquinoline;
organochlorine compound;
phenols;
secondary amino compound;
tertiary amino compound
anticoronaviral agent;
antimalarial;
drug allergen;
EC 2.1.1.8 (histamine N-methyltransferase) inhibitor;
non-steroidal anti-inflammatory drug;
prodrug
2012201212.0low000010
chloroquineaminoquinoline;
organochlorine compound;
secondary amino compound;
tertiary amino compound
anticoronaviral agent;
antimalarial;
antirheumatic drug;
autophagy inhibitor;
dermatologic drug
2006201613.2low100230
praziquantelisoquinolines201520159.0low000010
pyrimethamineaminopyrimidine;
monochlorobenzenes
antimalarial;
antiprotozoal drug;
EC 1.5.1.3 (dihydrofolate reductase) inhibitor
2006200717.5low000200
adamantaneadamantanes;
polycyclic alkane
200820209.8low000260
formal glycolcyclic acetal;
dioxolane
2013201311.0low000010
artemisininorganic peroxide;
sesquiterpene lactone
antimalarial;
plant metabolite
2004201714.6low000430
artemetherartemisinin derivative;
cyclic acetal;
organic peroxide;
semisynthetic derivative;
sesquiterpenoid
antimalarial2006201613.8low100320
atovaquonehydroxy-1,2-naphthoquinone2007200717.0low000100
artesunic acid2006201414.2low000220
piperaquineaminoquinoline;
N-arylpiperazine;
organochlorine compound
antimalarial200720219.5low600272
furamidine2006200817.0low000200
puromycinpuromycinsantiinfective agent;
antimicrobial agent;
antineoplastic agent;
EC 3.4.11.14 (cytosol alanyl aminopeptidase) inhibitor;
EC 3.4.14.2 (dipeptidyl-peptidase II) inhibitor;
nucleoside antibiotic;
protein synthesis inhibitor
201520159.0low000010
thapsigarginbutyrate ester;
organic heterotricyclic compound;
sesquiterpene lactone
calcium channel blocker;
EC 3.6.3.8 (Ca(2+)-transporting ATPase) inhibitor
2013201311.0low000010
artemisin2010201014.0low000100
sesquiterpenes2004200718.5low000600
tempoaminoxyls;
piperidines
catalyst;
ferroptosis inhibitor;
radical scavenger
2010201014.0low000100
lumefantrinefluorenes;
monochlorobenzenes;
secondary alcohol;
tertiary amine
antimalarial201620168.0low100010
cgp-56697201720215.0low200011
artenimol2012201610.0low000030
artemisone2012201411.0low000020
mefloquine202120213.0low100002
1,2,4-trioxane200820209.2low000130
oz 439201220208.0medium000060
deoxyartemisinin2007201015.5medium000200
hypoxanthinenucleobase analogue;
oxopurine;
purine nucleobase
fundamental metabolite2013201311.0low000010
ConditionIndicatedStudiesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
African Sleeping Sickness02009200915.0low000100
Disease Models, Animal02007201810.7low000120
Infections, Plasmodium02004202212.1high200681
Malaria02004202212.1high200681
Malaria, Falciparum02007202110.7medium700462
Malaria, Vivax02006201613.0low100110
Parasitemia02006200717.5low000200
Plasmodium falciparum Malaria02007202110.7medium700462
Plasmodium vivax Malaria02006201613.0low100110
Schistosoma mansoni Infection0201520159.0low000010
Schistosomiasis mansoni0201520159.0low000010
Sensitivity and Specificity02009200915.0low000100
Trypanosomiasis, African02009200915.0low000100

Safety/Toxicity (6)

ArticleYear
Efficacy and safety of fixed dose combination of arterolane maleate and piperaquine phosphate in comparison with chloroquine phosphate in children with acute uncomplicated
Journal of vector borne diseases, , Volume: 57, Issue:3
Assessment of Efficacy and Safety of Arterolane Maleate-Piperaquine Phosphate Dispersible Tablets in Comparison With Artemether-Lumefantrine Dispersible Tablets in Pediatric Patients With Acute Uncomplicated Plasmodium falciparum Malaria: A Phase 3, Rando
Clinical infectious diseases : an official publication of the Infectious Diseases Society of America, , Oct-30, Volume: 65, Issue:10
2017
Comparison of the safety and efficacy of fixed-dose combination of arterolane maleate and piperaquine phosphate with chloroquine in acute, uncomplicated Plasmodium vivax malaria: a phase III, multicentric, open-label study.
Malaria journal, , Jan-27, Volume: 15
2016
Efficacy and safety of fixed dose combination of arterolane maleate and piperaquine phosphate dispersible tablets in paediatric patients with acute uncomplicated Plasmodium falciparum malaria: a phase II, multicentric, open-label study.
Malaria journal, , Nov-25, Volume: 14
2015
Safety, tolerability and pharmacokinetic profile of single and multiple oral doses of arterolane (RBx11160) maleate in healthy subjects.
Journal of clinical pharmacology, , Volume: 54, Issue:4
2014
Comparative embryotoxicity of different antimalarial peroxides: in vitro study using the rat whole embryo culture model (WEC).
Reproductive toxicology (Elmsford, N.Y.), , Volume: 30, Issue:4
2010

Pharmacokinetics (3)

ArticleYear
Endoperoxide Drug Cross-Resistance Patterns for Plasmodium falciparum Exhibiting an Artemisinin Delayed-Clearance Phenotype.
Antimicrobial agents and chemotherapy, , Volume: 60, Issue:11
2016
Safety, tolerability and pharmacokinetic profile of single and multiple oral doses of arterolane (RBx11160) maleate in healthy subjects.
Journal of clinical pharmacology, , Volume: 54, Issue:4
2014
Pharmacokinetics and pharmacodynamics of arterolane maleate following multiple oral doses in adult patients with P. falciparum malaria.
Journal of clinical pharmacology, , Volume: 51, Issue:11
2011

Bioavailability (3)

ArticleYear
Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3
2017
Comparison of the safety and efficacy of fixed-dose combination of arterolane maleate and piperaquine phosphate with chloroquine in acute, uncomplicated Plasmodium vivax malaria: a phase III, multicentric, open-label study.
Malaria journal, , Jan-27, Volume: 15
2016
Identification of an antimalarial synthetic trioxolane drug development candidate.
Nature, , Aug-19, Volume: 430, Issue:7002
2004

Dosage (2)

ArticleYear
Assessment of Efficacy and Safety of Arterolane Maleate-Piperaquine Phosphate Dispersible Tablets in Comparison With Artemether-Lumefantrine Dispersible Tablets in Pediatric Patients With Acute Uncomplicated Plasmodium falciparum Malaria: A Phase 3, Rando
Clinical infectious diseases : an official publication of the Infectious Diseases Society of America, , Oct-30, Volume: 65, Issue:10
2017
Safety, tolerability and pharmacokinetic profile of single and multiple oral doses of arterolane (RBx11160) maleate in healthy subjects.
Journal of clinical pharmacology, , Volume: 54, Issue:4
2014