Page last updated: 2024-11-09

stk295900

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

Cross-References

ID SourceID
PubMed CID1365597
CHEMBL ID531018
SCHEMBL ID9862039
SCHEMBL ID419961
MeSH IDM0586270

Synonyms (22)

Synonym
CBMICRO_033003
OPREA1_365596
OPREA1_668353
BIM-0032961.P001
STK295900 ,
4,4'-(1h,3'h-5,5'-bibenzimidazole-2,2'-diyl)dianiline
TCMDC-123459 ,
sj000111341
gnf-pf-2870 ,
CHEMBL531018 ,
SCHEMBL9862039
4-[6-[2-(4-aminophenyl)-3h-benzimidazol-5-yl]-1h-benzimidazol-2-yl]aniline
AKOS003242168
AKOS004912801
SCHEMBL419961
2,2'-di(p-aminophenyl)-5,5'-bibenzimidazole
cambridge id 5181312
4402-17-9
5,5'-bis[2-(4-aminophenyl)-1h-1,3-benzimidazol]
bdbm50134735
4,4'-(1h,3'h-5,5'-bibenzo[d]imidazole-2,2'-diyl)dianiline
benzenamine, 4,4'-[5,5'-bi-1h-benzimidazole]-2,2'-diylbis-

Research Excerpts

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]

Protein Targets (4)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
DNA gyrase subunit BStaphylococcus aureusIC50 (µMol)0.30000.00401.50207.7000AID1270519
DNA gyrase subunit AStaphylococcus aureusIC50 (µMol)0.30000.00401.98397.7000AID1270519
DNA gyrase subunit BMycobacterium tuberculosis H37RvIC50 (µMol)11.30000.01502.467610.0000AID1270522
DNA gyrase subunit AMycobacterium tuberculosis H37RvIC50 (µMol)11.30000.01503.477310.0000AID1270522
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (46)

Assay IDTitleYearJournalArticle
AID1384038Antimycobacterial activity against Mycobacterium tuberculosis H37Rv in logarithmic phase2018European journal of medicinal chemistry, Apr-25, Volume: 150Recent advances of imidazole-containing derivatives as anti-tubercular agents.
AID449721ST_JUDE: Cytotoxicity against Plasmodium falciparum SB-A62010Nature, May-20, Volume: 465, Issue:7296
Chemical genetics of Plasmodium falciparum.
AID1270522Inhibition of Mycobacterium tuberculosis H37Rv DNA gyrase supercoiling activity2015MedChemComm, Aug-05, Volume: 6, Issue:8
The discovery of a novel antibiotic for the treatment of
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.
AID449709ST_JUDE: Cytotoxicity against Plasmodium falciparum 3D72010Nature, May-20, Volume: 465, Issue:7296
Chemical genetics of Plasmodium falciparum.
AID449713ST_JUDE: Cytotoxicity using luciferase to measure ATP as an indicator of the viability of Trypanosoma brucei2010Nature, May-20, Volume: 465, Issue:7296
Chemical genetics of Plasmodium falciparum.
AID449720ST_JUDE: Cytotoxicity against Plasmodium falciparum W22010Nature, May-20, Volume: 465, Issue:7296
Chemical genetics of Plasmodium falciparum.
AID449718ST_JUDE: Cytotoxicity using luciferase to measure ATP as an indicator of the viability of human Burkitt''s lymphoma lymphoblast cells (Raji)2010Nature, May-20, Volume: 465, Issue:7296
Chemical genetics of Plasmodium falciparum.
AID1270514Antibacterial activity against clinical isolates of Staphylococcus aureus EMRSA-16 assessed as growth inhibition after 20 hrs by broth dilution method2015MedChemComm, Aug-05, Volume: 6, Issue:8
The discovery of a novel antibiotic for the treatment of
AID1270516Antibacterial activity against Clostridium difficile R20291 assessed as growth inhibition2015MedChemComm, Aug-05, Volume: 6, Issue:8
The discovery of a novel antibiotic for the treatment of
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.
AID449716ST_JUDE: Cytotoxicity using luciferase to measure ATP as an indicator of the viability of human epithelial hepatocellular carcinoma cells (HepG2)2010Nature, May-20, Volume: 465, Issue:7296
Chemical genetics of Plasmodium falciparum.
AID1270523Inhibition of Escherichia coli topoisomerase 4-mediated DNA decatenation activity2015MedChemComm, Aug-05, Volume: 6, Issue:8
The discovery of a novel antibiotic for the treatment of
AID1270513Antibacterial activity against Staphylococcus aureus ATCC 29213 assessed as growth inhibition after 20 hrs by broth dilution method2015MedChemComm, Aug-05, Volume: 6, Issue:8
The discovery of a novel antibiotic for the treatment of
AID1270515Antibacterial activity against Clostridium difficile CD 630 assessed as growth inhibition2015MedChemComm, Aug-05, Volume: 6, Issue:8
The discovery of a novel antibiotic for the treatment of
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.
AID449712ST_JUDE: Growth inhibition of to Toxoplasma gondii, in human U-2OS cells, as measured by luciferase.2010Nature, May-20, Volume: 465, Issue:7296
Chemical genetics of Plasmodium falciparum.
AID449722ST_JUDE: Cytotoxicity against Plasmodium falciparum D10 transfected with yeast DHOD2010Nature, May-20, Volume: 465, Issue:7296
Chemical genetics of Plasmodium falciparum.
AID449715ST_JUDE: Cytotoxicity using luciferase to measure ATP as an indicator of the viability of human foreskin fibroblast cells (BJ)2010Nature, May-20, Volume: 465, Issue:7296
Chemical genetics of Plasmodium falciparum.
AID1270525Inhibition of Escherichia coli topoisomerase 4-mediated DNA relaxation activity2015MedChemComm, Aug-05, Volume: 6, Issue:8
The discovery of a novel antibiotic for the treatment of
AID1270519Inhibition of Staphylococcus aureus DNA gyrase assessed as reduction in enzyme-catalyzed supercoiling of relaxed circular pBR322 DNA incubated for 30 mins by agarose gel electrophoresis2015MedChemComm, Aug-05, Volume: 6, Issue:8
The discovery of a novel antibiotic for the treatment of
AID1270512Antibacterial activity against Escherichia coli MC 1061 assessed as growth inhibition2015MedChemComm, Aug-05, Volume: 6, Issue:8
The discovery of a novel antibiotic for the treatment of
AID1270520Inhibition of Escherichia coli DNA gyrase supercoiling activity2015MedChemComm, Aug-05, Volume: 6, Issue:8
The discovery of a novel antibiotic for the treatment of
AID449711ST_JUDE: Cytotoxicity against Plasmodium falciparum V1/S2010Nature, May-20, Volume: 465, Issue:7296
Chemical genetics of Plasmodium falciparum.
AID1270524Inhibition of Staphylococcus aureus topoisomerase 4 assessed as inhibition of decatenation of catenated kinetoplast DNA after 30 mins by agarose gel electrophoresis2015MedChemComm, Aug-05, Volume: 6, Issue:8
The discovery of a novel antibiotic for the treatment of
AID1384039Antimycobacterial activity against Mycobacterium tuberculosis H37Rv in hypoxia-induced latent phase2018European journal of medicinal chemistry, Apr-25, Volume: 150Recent advances of imidazole-containing derivatives as anti-tubercular agents.
AID1270511Antibacterial activity against Escherichia coli NCTC 10418 assessed as growth inhibition2015MedChemComm, Aug-05, Volume: 6, Issue:8
The discovery of a novel antibiotic for the treatment of
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.
AID449717ST_JUDE: Cytotoxicity using luciferase to measure ATP as an indicator of the viability of human epithelial embryonic kidney cells (HEK293)2010Nature, May-20, Volume: 465, Issue:7296
Chemical genetics of Plasmodium falciparum.
AID449714ST_JUDE: Cytotoxicity using Alamar Blue to measure viability of Leishmania major2010Nature, May-20, Volume: 465, Issue:7296
Chemical genetics of Plasmodium falciparum.
AID1270518Antibacterial activity against Mycobacterium tuberculosis H37Rv hypoxia-induced latency form by spot culture growth inhibition assay2015MedChemComm, Aug-05, Volume: 6, Issue:8
The discovery of a novel antibiotic for the treatment of
AID449719ST_JUDE: Cytotoxicity against Plasmodium falciparum Dd22010Nature, May-20, Volume: 465, Issue:7296
Chemical genetics of Plasmodium falciparum.
AID1270521Inhibition of Clostridium difficile DNA gyrase supercoiling activity2015MedChemComm, Aug-05, Volume: 6, Issue:8
The discovery of a novel antibiotic for the treatment of
AID449708ST_JUDE: Plasmodium falciparum K1 EC50 (uM) as measured by SYBR green dye2010Nature, May-20, Volume: 465, Issue:7296
Chemical genetics of Plasmodium falciparum.
AID449710ST_JUDE: Cytotoxicity against Plasmodium falciparum K12010Nature, May-20, Volume: 465, Issue:7296
Chemical genetics of Plasmodium falciparum.
AID1270517Antibacterial activity against Mycobacterium tuberculosis H37Rv logarithmic phase forms by spot culture growth inhibition assay2015MedChemComm, Aug-05, Volume: 6, Issue:8
The discovery of a novel antibiotic for the treatment of
AID449707ST_JUDE: Plasmodium falciparum 3D7 EC50 (uM) as measured by SYBR green dye2010Nature, May-20, Volume: 465, Issue:7296
Chemical genetics of Plasmodium falciparum.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).2014Journal of biomolecular screening, Jul, Volume: 19, Issue:6
A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).
AID1159588Biochemical screen of P. falciparum CDPK42016PloS one, , Volume: 11, Issue:3
Biochemical Screening of Five Protein Kinases from Plasmodium falciparum against 14,000 Cell-Active Compounds.
AID1159586Biochemical screen of P. falciparum PK62016PloS one, , Volume: 11, Issue:3
Biochemical Screening of Five Protein Kinases from Plasmodium falciparum against 14,000 Cell-Active Compounds.
AID1159589Biochemical screen of P. falciparum MAPK22016PloS one, , Volume: 11, Issue:3
Biochemical Screening of Five Protein Kinases from Plasmodium falciparum against 14,000 Cell-Active Compounds.
AID1159587Biochemical screen of P. falciparum PK72016PloS one, , Volume: 11, Issue:3
Biochemical Screening of Five Protein Kinases from Plasmodium falciparum against 14,000 Cell-Active Compounds.
AID1159585Biochemical screen of P. falciparum CDPK12016PloS one, , Volume: 11, Issue:3
Biochemical Screening of Five Protein Kinases from Plasmodium falciparum against 14,000 Cell-Active Compounds.
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.
AID1159537qHTS screening for TAG (triacylglycerol) accumulators in algae2017Plant physiology, Aug, Volume: 174, Issue:4
Identification and Metabolite Profiling of Chemical Activators of Lipid Accumulation in Green Algae.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (9)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's1 (11.11)29.6817
2010's7 (77.78)24.3611
2020's1 (11.11)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.62

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index12.62 (24.57)
Research Supply Index2.30 (2.92)
Research Growth Index4.92 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.62)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews2 (22.22%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other7 (77.78%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]