Page last updated: 2024-11-07

cl 246738

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

Description

3,6-bis(2-piperidinoethoxy)acridine trihydrochloride: immunomodulator; structure given in first source; RN given for tri-HCl [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID133712
CHEMBL ID576799
SCHEMBL ID9827046
MeSH IDM0132437

Synonyms (21)

Synonym
3,6-bis[2-(1-piperidyl)ethoxy]acridine
3,6-bis(2-piperidinoethoxy)acridine trihydrochloride
acridine, 3,6-bis[2-(1-piperidinyl)ethoxy]-
81541-32-4
3,6-bis(2-piperidinoethoxy)acridine
cl 246,738
gnf-pf-1482 ,
CHEMBL576799
3,6-bis(2-piperidin-1-ylethoxy)acridine
unii-ip2pou1mkn
acridine, 3,6-bis(2-(1-piperidinyl)ethoxy)-
ip2pou1mkn ,
cl-246738 free base
SCHEMBL9827046
DTXSID40231194
QKPASNYRBWHSBK-UHFFFAOYSA-N
cl-246738
3,6-bis(2-piperidinoethoxy) acridine
3,6-bis(2-(1-piperidinyl)ethoxy)acridine
cl-2l
3,6-bis(2-(piperidin-1-yl)ethoxy)acridine

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" Toxic effects of the drug at high doses included nausea, diarrhoea and decreased levels of consciousness."( A phase I study of immunostimulation and toxicity in patients with colorectal carcinoma using the immunomodulator 3,6-bis(2-piperidinoethoxy) acridine trihydrochloride (CL 246738).
Dickinson, A; Halcrow, P; Hales, J; Harris, AL; Lawrence, GF; Lennard, TW; McDonald, M; Shenton, BK; Taylor, RM; Wolstencroft, R, 1989
)
0.28

Bioavailability

ExcerptReferenceRelevance
" The orally bioavailable lead imidazolopiperazine confers complete causal prophylactic protection (15 milligrams/kilogram) in rodent models of malaria and shows potent in vivo blood-stage therapeutic activity."( Imaging of Plasmodium liver stages to drive next-generation antimalarial drug discovery.
Barnes, SW; Bonamy, GM; Bopp, SE; Borboa, R; Bright, AT; Chatterjee, A; Che, J; Cohen, S; Dharia, NV; Diagana, TT; Fidock, DA; Froissard, P; Gagaring, K; Gettayacamin, M; Glynne, RJ; Gordon, P; Groessl, T; Kato, N; Kuhen, KL; Lee, MC; Mazier, D; McNamara, CW; Meister, S; Nagle, A; Nam, TG; Plouffe, DM; Richmond, W; Roland, J; Rottmann, M; Sattabongkot, J; Schultz, PG; Tuntland, T; Walker, JR; Winzeler, EA; Wu, T; Zhou, B; Zhou, Y, 2011
)
0.37
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (5)

Assay IDTitleYearJournalArticle
AID449704NOVARTIS: Inhibition of Plasmodium falciparum W2 (drug-resistant) proliferation in erythrocyte-based infection assay2008Proceedings of the National Academy of Sciences of the United States of America, Jul-01, Volume: 105, Issue:26
In silico activity profiling reveals the mechanism of action of antimalarials discovered in a high-throughput screen.
AID449703NOVARTIS: Inhibition of Plasmodium falciparum 3D7 (drug-susceptible) proliferation in erythrocyte-based infection assay 2008Proceedings of the National Academy of Sciences of the United States of America, Jul-01, Volume: 105, Issue:26
In silico activity profiling reveals the mechanism of action of antimalarials discovered in a high-throughput screen.
AID449706NOVARTIS: Inhibition Frequency Index (IFI) - the number of HTS assays where a compound showed > 50% inhibition/induction, expressed as a percentage of the number of assays in which the compound was tested.2008Proceedings of the National Academy of Sciences of the United States of America, Jul-01, Volume: 105, Issue:26
In silico activity profiling reveals the mechanism of action of antimalarials discovered in a high-throughput screen.
AID449705NOVARTIS: Cytotoxicity against human hepatocellular carcinoma cell line (Huh7)2008Proceedings of the National Academy of Sciences of the United States of America, Jul-01, Volume: 105, Issue:26
In silico activity profiling reveals the mechanism of action of antimalarials discovered in a high-throughput screen.
AID602156Novartis GNF Liver Stage Dataset: Malariabox Annotation2011Science (New York, N.Y.), Dec-09, Volume: 334, Issue:6061
Imaging of Plasmodium liver stages to drive next-generation antimalarial drug discovery.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (17)

TimeframeStudies, This Drug (%)All Drugs %
pre-19908 (47.06)18.7374
1990's7 (41.18)18.2507
2000's1 (5.88)29.6817
2010's1 (5.88)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other18 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]