Compounds > genz10850
Page last updated: 2024-11-08

genz10850

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 CID447767
CHEMBL ID216579
SCHEMBL ID7664894
MeSH IDM0451661

Synonyms (12)

Synonym
piperazine, p3
bdbm25796
genz-10850
[4-(9h-fluoren-9-yl)piperazin-1-yl]-(1h-indol-5-yl)methanone
[4-(9h-fluoren-9-yl)-piperazin-1-yl]-(1h-indol-5-yl)-methanone
5-{[4-(9h-fluoren-9-yl)piperazin-1-yl]carbonyl}-1h-indole
GEQ ,
DB04289
CHEMBL216579
SCHEMBL7664894
YYMZSGIXLQPFAC-UHFFFAOYSA-N
Q27095111
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (1)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Enoyl-[acyl-carrier-protein] reductase [NADH]Mycobacterium tuberculosis H37RvIC50 (µMol)0.18000.03002.286410.0000AID1339826; AID1352697; AID1798583; AID301095
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (27)

Assay IDTitleYearJournalArticle
AID1060595Cytotoxicity against human HCT116 cells after 4 days by WST-1 assay2014European journal of medicinal chemistry, Jan, Volume: 71Synthesis of 3-heteryl substituted pyrrolidine-2,5-diones via catalytic Michael reaction and evaluation of their inhibitory activity against InhA and Mycobacterium tuberculosis.
AID1241972Ratio of MIC for Mycobacterium tuberculosis H37Rv in absence of CCCP to MIC for Mycobacterium tuberculosis H37Rv in presence of CCCP2015European journal of medicinal chemistry, Aug-28, Volume: 101Design, synthesis and evaluation of new GEQ derivatives as inhibitors of InhA enzyme and Mycobacterium tuberculosis growth.
AID273125Inhibition of Mycobacterium tuberculosis InhA at 15 uM2006Journal of medicinal chemistry, Oct-19, Volume: 49, Issue:21
Pyrrolidine carboxamides as a novel class of inhibitors of enoyl acyl carrier protein reductase from Mycobacterium tuberculosis.
AID1054533Inhibition of Mycobacterium tuberculosis InhA expressed in Escherichia coli using trans-2-dodecenoyl-coenzyme-A as substrate at 50 uM2013European journal of medicinal chemistry, , Volume: 70Design, chemical synthesis of 3-(9H-fluoren-9-yl)pyrrolidine-2,5-dione derivatives and biological activity against enoyl-ACP reductase (InhA) and Mycobacterium tuberculosis.
AID1241974Antimycobacterial activity against Mycobacterium tuberculosis by CFU counting method2015European journal of medicinal chemistry, Aug-28, Volume: 101Design, synthesis and evaluation of new GEQ derivatives as inhibitors of InhA enzyme and Mycobacterium tuberculosis growth.
AID1241967Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 21 days by microbroth dilution method2015European journal of medicinal chemistry, Aug-28, Volume: 101Design, synthesis and evaluation of new GEQ derivatives as inhibitors of InhA enzyme and Mycobacterium tuberculosis growth.
AID1168879Antimalarial activity against Plasmodium falciparum Dd22014Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21
Synthesis and evaluation of the antiplasmodial activity of novel indeno[2,1-c]quinoline derivatives.
AID1241964Inhibition of Mycobacterium tuberculosis His6-tagged InhA expressed in Escherichia coli BL21 using 2-trans-dodecenoyl-CoA as substrate assessed as conversion of NADH to NAD+2015European journal of medicinal chemistry, Aug-28, Volume: 101Design, synthesis and evaluation of new GEQ derivatives as inhibitors of InhA enzyme and Mycobacterium tuberculosis growth.
AID1054532Antimicrobial activity against Mycobacterium tuberculosis H37Rv by two-fold serial dilution method2013European journal of medicinal chemistry, , Volume: 70Design, chemical synthesis of 3-(9H-fluoren-9-yl)pyrrolidine-2,5-dione derivatives and biological activity against enoyl-ACP reductase (InhA) and Mycobacterium tuberculosis.
AID1060594Inhibition of Mycobacterium tuberculosis recombinant His6x-tagged InhA expressed in Escherichia coli BL21 at 50 uM2014European journal of medicinal chemistry, Jan, Volume: 71Synthesis of 3-heteryl substituted pyrrolidine-2,5-diones via catalytic Michael reaction and evaluation of their inhibitory activity against InhA and Mycobacterium tuberculosis.
AID1241962Inhibition of Mycobacterium tuberculosis His6-tagged InhA expressed in Escherichia coli BL21 using 2-trans-dodecenoyl-CoA as substrate assessed as conversion of NADH to NAD+ at 50 uM relative to control2015European journal of medicinal chemistry, Aug-28, Volume: 101Design, synthesis and evaluation of new GEQ derivatives as inhibitors of InhA enzyme and Mycobacterium tuberculosis growth.
AID1241971Ratio of MIC for Mycobacterium tuberculosis H37Rv in absence of verapamil to MIC for Mycobacterium tuberculosis H37Rv in presence of verapamil2015European journal of medicinal chemistry, Aug-28, Volume: 101Design, synthesis and evaluation of new GEQ derivatives as inhibitors of InhA enzyme and Mycobacterium tuberculosis growth.
AID1591632Inhibition of Mycobacterium tuberculosis InhA at 50 uM using DDCoA as substrate relative to control2019Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16
Discovery of novel N-methyl carbazole tethered rhodanine derivatives as direct inhibitors of Mycobacterium tuberculosis InhA.
AID1241975Antimycobacterial activity against Mycobacterium tuberculosis by Alamar blue assay2015European journal of medicinal chemistry, Aug-28, Volume: 101Design, synthesis and evaluation of new GEQ derivatives as inhibitors of InhA enzyme and Mycobacterium tuberculosis growth.
AID1241970Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 21 days by microbroth dilution method in presence of 7.5 ug/ml efflux pump inhibitor CCCP2015European journal of medicinal chemistry, Aug-28, Volume: 101Design, synthesis and evaluation of new GEQ derivatives as inhibitors of InhA enzyme and Mycobacterium tuberculosis growth.
AID1241963Inhibition of Mycobacterium tuberculosis His6-tagged InhA expressed in Escherichia coli BL21 using 2-trans-dodecenoyl-CoA as substrate assessed as conversion of NADH to NAD+ at 10 uM relative to control2015European journal of medicinal chemistry, Aug-28, Volume: 101Design, synthesis and evaluation of new GEQ derivatives as inhibitors of InhA enzyme and Mycobacterium tuberculosis growth.
AID1241968Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 21 days by microbroth dilution method in presence of 3 ug/ml efflux pump inhibitor reserpine2015European journal of medicinal chemistry, Aug-28, Volume: 101Design, synthesis and evaluation of new GEQ derivatives as inhibitors of InhA enzyme and Mycobacterium tuberculosis growth.
AID504180Antitubercular activity against Mycobacterium tuberculosis H37Rv after 7 days2010Bioorganic & medicinal chemistry, Sep-15, Volume: 18, Issue:18
Identification of novel antitubercular compounds through hybrid virtual screening approach.
AID301095Inhibition of Mycobacterium tuberculosis InhA2007Bioorganic & medicinal chemistry, Nov-01, Volume: 15, Issue:21
Inhibition of the Mycobacterium tuberculosis enoyl acyl carrier protein reductase InhA by arylamides.
AID1591635Antimycobacterial activity against Mycobacterium tuberculosis H37Rv incubated for 5 days under aerobic condition by fluorescence assay2019Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16
Discovery of novel N-methyl carbazole tethered rhodanine derivatives as direct inhibitors of Mycobacterium tuberculosis InhA.
AID1168868Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 infected in human type A-positive red blood cells assessed as growth inhibition after 72 hrs by spectrophotometrically2014Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21
Synthesis and evaluation of the antiplasmodial activity of novel indeno[2,1-c]quinoline derivatives.
AID301096Inhibition of Mycobacterium tuberculosis InhA at 15 uM2007Bioorganic & medicinal chemistry, Nov-01, Volume: 15, Issue:21
Inhibition of the Mycobacterium tuberculosis enoyl acyl carrier protein reductase InhA by arylamides.
AID1352697Inhibition of Mycobacterium tuberculosis InhA using trans-2-decenoyl-CoA as substrate2018European journal of medicinal chemistry, Feb-25, Volume: 146An overview on crystal structures of InhA protein: Apo-form, in complex with its natural ligands and inhibitors.
AID1060593Antimicrobial activity against Mycobacterium tuberculosis H37Rv after 21 days by micro-broth dilution method2014European journal of medicinal chemistry, Jan, Volume: 71Synthesis of 3-heteryl substituted pyrrolidine-2,5-diones via catalytic Michael reaction and evaluation of their inhibitory activity against InhA and Mycobacterium tuberculosis.
AID1241969Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 21 days by microbroth dilution method in presence of 40 ug/ml efflux pump inhibitor verapamil2015European journal of medicinal chemistry, Aug-28, Volume: 101Design, synthesis and evaluation of new GEQ derivatives as inhibitors of InhA enzyme and Mycobacterium tuberculosis growth.
AID1060592Cytotoxicity against human GM637 cells after 4 days by WST-1 assay2014European journal of medicinal chemistry, Jan, Volume: 71Synthesis of 3-heteryl substituted pyrrolidine-2,5-diones via catalytic Michael reaction and evaluation of their inhibitory activity against InhA and Mycobacterium tuberculosis.
AID1798583InhA Enzyme Inhibition Assay from Article 10.1016/j.bmc.2007.08.013: \\Inhibition of the Mycobacterium tuberculosis enoyl acyl carrier protein reductase InhA by arylamides.\\2007Bioorganic & medicinal chemistry, Nov-01, Volume: 15, Issue:21
Inhibition of the Mycobacterium tuberculosis enoyl acyl carrier protein reductase InhA by arylamides.
[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's2 (22.22)29.6817
2010's7 (77.78)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.43

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 Index12.43 (24.57)
Research Supply Index2.30 (2.92)
Research Growth Index4.73 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.43)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (11.11%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other8 (88.89%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
chloroquine
Chloroquine: The prototypical antimalarial agent with a mechanism that is not well understood. It has also been used to treat rheumatoid arthritis, systemic lupus erythematosus, and in the systemic therapy of amebic liver abscesses.. chloroquine : An aminoquinoline that is quinoline which is substituted at position 4 by a [5-(diethylamino)pentan-2-yl]amino group at at position 7 by chlorine. It is used for the treatment of malaria, hepatic amoebiasis, lupus erythematosus, light-sensitive skin eruptions, and rheumatoid arthritis.		2.110aminoquinoline;
organochlorine compound;
secondary amino compound;
tertiary amino compound		anticoronaviral agent;
antimalarial;
antirheumatic drug;
autophagy inhibitor;
dermatologic drug
isoniazid
Hydra: A genus of freshwater polyps in the family Hydridae, order Hydroida, class HYDROZOA. They are of special interest because of their complex organization and because their adult organization corresponds roughly to the gastrula of higher animals.. hydrazide : Compounds derived from oxoacids RkE(=O)l(OH)m (l =/= 0) by replacing -OH by -NRNR2 (R groups are commonly H). (IUPAC).		3.9130carbohydrazideantitubercular agent;
drug allergen
triclosan
[no description available]		3.6320aromatic ether;
dichlorobenzene;
monochlorobenzenes;
phenols		antibacterial agent;
antimalarial;
drug allergen;
EC 1.3.1.9 [enoyl-[acyl-carrier-protein] reductase (NADH)] inhibitor;
EC 1.5.1.3 (dihydrofolate reductase) inhibitor;
fungicide;
persistent organic pollutant;
xenobiotic
4-(9H-fluoren-9-yl)-N-phenyl-1-piperazinecarboxamide
[no description available]		2.1110fluorenes
lumefantrine
Lumefantrine: A fluorene derivative that is used in combination with ARTEMETHER for the treatment of MALARIA (see ARTEMETHER-LUMEFANTRINE DRUG COMBINATION).. lumefantrine : A member of the class of fluorenes that is 9-(p-chlorobenzylidene)-9H-fluorene which is substitutec by chlorine at positions 2 and 7, and by a 2-(dibutylamino)-1-hydroxyethyl group at position 4. An antimalarial drug used in combination with artemether for the treatment of multi-drug resistant strains of falciparum malaria.		2.110fluorenes;
monochlorobenzenes;
secondary alcohol;
tertiary amine		antimalarial
rifampin
Rifampin: A semisynthetic antibiotic produced from Streptomyces mediterranei. It has a broad antibacterial spectrum, including activity against several forms of Mycobacterium. In susceptible organisms it inhibits DNA-dependent RNA polymerase activity by forming a stable complex with the enzyme. It thus suppresses the initiation of RNA synthesis. Rifampin is bactericidal, and acts on both intracellular and extracellular organisms. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p1160)		2.0510cyclic ketal;
hydrazone;
N-iminopiperazine;
N-methylpiperazine;
rifamycins;
semisynthetic derivative;
zwitterion		angiogenesis inhibitor;
antiamoebic agent;
antineoplastic agent;
antitubercular agent;
DNA synthesis inhibitor;
EC 2.7.7.6 (RNA polymerase) inhibitor;
Escherichia coli metabolite;
geroprotector;
leprostatic drug;
neuroprotective agent;
pregnane X receptor agonist;
protein synthesis inhibitor
ConditionIndicatedRelationship StrengthStudiesTrials
Koch's Disease
[description not available]		02.110
Tuberculosis
Any of the infectious diseases of man and other animals caused by species of MYCOBACTERIUM TUBERCULOSIS.		02.110