Page last updated: 2024-11-08

abt 492

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

Description

WQ 3034: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID487101
CHEMBL ID2105637
SCHEMBL ID294694
MeSH IDM0454757

Synonyms (59)

Synonym
delafloxacin ,
rx-3341
a-319492
abt 492
1-(6-amino-3,5-difluoro-2-pyridyl)-8-chloro-6-fluoro-7-(3-hydroxyazetidin-1-yl)-4-oxo-quinoline-3-carboxylic acid
abt-492 ,
3-quinolinecarboxylic acid, 1-(6-amino-3,5-difluoro-2-pyridinyl)-8-chloro-6-fluoro-1,4-dihydro-7-(3-hydroxy-1-azetidinyl)-4-oxo-
wq-3034
D09330
delafloxacin (usan)
189279-58-1
1-(6-amino-3,5-difluoropyridin-2-yl)-8-chloro-6-fluoro-7-(3-hydroxyazetidin-1-yl)-4-oxoquinoline-3-carboxylic acid
CHEMBL2105637
baxdela
delafloxacin [usan:inn]
wq 3034
abt492
6315412yvf ,
delafloxacinum
unii-6315412yvf
1-(6-amino-3,5-difluoropyridin-2-yl)-8-chloro-6-fluoro-7-(3-hydroxyazetidin-1-yl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
S1553
delafloxacin [usan]
delafloxacin [mi]
delafloxacin [who-dd]
delafloxacin [inn]
SCHEMBL294694
DYDCPNMLZGFQTM-UHFFFAOYSA-N
1-(6-amino-3,5-difluoropyridine-2-yl)-8-chloro-6-fluoro-7-(3-hydroxyazetidine-1-yl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
AC-30739
FT-0697895
DTXSID40172331 ,
AKOS027270087
HY-14814
CS-1478
AS-75147
NCGC00390187-01
delafloxacin, >=98% (hplc)
delafloxacinabt-492
DB11943
Q5253067
bdbm50560872
EX-A2331
rx-3341; wq-3034; abt492; delafloxacin
SB16746
AMY4217
quofenix
NCGC00390187-02
abbott 492
gtpl10799
C73623
abt-492(delafloxacin, rx-3341, wq-3034)
189279-58-1, 339591-82-1 (sodium salt)
delafloxacin 100 microg/ml in acetonitrile
delafloxacino
dtxcid9094822
delafloxacine
j01ma23
EN300-7380878

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" Frequency of treatment-emergent adverse events in the delafloxacin and vancomycin/aztreonam groups was similar."( Efficacy and safety of delafloxacin compared with vancomycin plus aztreonam for acute bacterial skin and skin structure infections: a Phase 3, double-blind, randomized study.
Cammarata, S; Farley, B; Gardovskis, J; Lawrence, L; Ling, R; Pullman, J; Quintas, M; Sun, E, 2017
)
0.46
" Frequency of treatment-emergent adverse events between the groups was similar."( A Comparison of the Efficacy and Safety of Intravenous Followed by Oral Delafloxacin With Vancomycin Plus Aztreonam for the Treatment of Acute Bacterial Skin and Skin Structure Infections: A Phase 3, Multinational, Double-Blind, Randomized Study.
Cammarata, S; Cruz-Saldariagga, M; Lawrence, L; Liang, S; McManus, A; O'Riordan, W; Poromanski, I; Quintas, M; Teras, J, 2018
)
0.48
" Adverse events were monitored throughout the study."( Lack of phototoxicity potential with delafloxacin in healthy male and female subjects: comparison to lomefloxacin.
Cammarata, S; Dawe, RS; Duffy, E; Ferguson, J; Ibbotson, S; Lawrence, L; Paulson, S, 2018
)
0.48
" Adverse events (AEs) associated with the fluoroquinolones are well defined and a prospective part of the development process."( Analysis of Pooled Phase 3 Safety Data for Delafloxacin in Acute Bacterial Skin and Skin Structure Infections.
Bassetti, M; Hooper, D; Tillotson, G, 2019
)
0.51
"DLX was safe and well-tolerated in the pooled phase 3 ABSSSI trial population of 741 subjects."( Analysis of Pooled Phase 3 Safety Data for Delafloxacin in Acute Bacterial Skin and Skin Structure Infections.
Bassetti, M; Hooper, D; Tillotson, G, 2019
)
0.51
" Gastrointestinal adverse events were common with 900-mg of delafloxacin and typically included mild to moderate diarrhea, flatulence, nausea, and vomiting."( Efficacy and Safety of Single-Dose Oral Delafloxacin Compared With Intramuscular Ceftriaxone for Uncomplicated Gonorrhea Treatment: An Open-Label, Noninferiority, Phase 3, Multicenter, Randomized Study.
Cammarata, S; Golden, MR; Henry, E; Hook, EW; Nenninger, A; Swerdlow, J; Taylor, SN; Tseng, C; Workowski, KA, 2019
)
0.51

Pharmacokinetics

ExcerptReferenceRelevance
" We therefore compared the in vitro pharmacodynamic activity of ABT-492 to that of levofloxacin, an antibiotic commonly used for the treatment of pneumonia, through MIC determination and time-kill kinetic analysis."( In vitro pharmacodynamic activities of ABT-492, a novel quinolone, compared to those of levofloxacin against Streptococcus pneumoniae, Haemophilus influenzae, and Moraxella catarrhalis.
Danziger, LH; Gunderson, SM; Hayes, RA; Quinn, JP, 2004
)
0.32
"The objective of this report was to determine the pharmacokinetic properties, safety, and tolerability of single and multiple doses of intravenous delafloxacin."( Safety, Tolerability, and Pharmacokinetic Properties of Intravenous Delafloxacin After Single and Multiple Doses in Healthy Volunteers.
Benedict, M; Cammarata, S; Hoover, R; Hunt, T; Lawrence, L; Paulson, SK; Sun, E, 2016
)
0.43
" Serial blood samples were collected, and plasma pharmacokinetic parameters of delafloxacin were calculated."( Safety, Tolerability, and Pharmacokinetic Properties of Intravenous Delafloxacin After Single and Multiple Doses in Healthy Volunteers.
Benedict, M; Cammarata, S; Hoover, R; Hunt, T; Lawrence, L; Paulson, SK; Sun, E, 2016
)
0.43
"Delafloxacin Cmax values increased proportionally with increasing single IV dose for the dose range of 300 to 1200 mg, whereas the AUC values increased more than proportionally to dose for the same dose range."( Safety, Tolerability, and Pharmacokinetic Properties of Intravenous Delafloxacin After Single and Multiple Doses in Healthy Volunteers.
Benedict, M; Cammarata, S; Hoover, R; Hunt, T; Lawrence, L; Paulson, SK; Sun, E, 2016
)
0.43
" This review focuses on recent advances concerning quinolones and fluoroquinolones, we will be summarising chemical structure, mode of action, pharmacokinetic properties and toxicity."( Chemical structure and pharmacokinetics of novel quinolone agents represented by avarofloxacin, delafloxacin, finafloxacin, zabofloxacin and nemonoxacin.
Domokos, J; Kocsis, B; Szabo, D, 2016
)
0.43
" Full pharmacokinetic profiles were obtained on days 1 and 8 (midazolam and 1-hydroxymidazolam) and days 3 and 7 (delafloxacin)."( The Pharmacokinetics of the CYP3A Substrate Midazolam After Steady-state Dosing of Delafloxacin.
Cammarata, SK; Hoover, R; Lawrence, LE; Paulson, SK; Quintas, M; Wood-Horrall, RN, 2017
)
0.46
" Areas covered: In this drug evaluation, the Authors have reviewed the pharmacokinetic and pharmacodynamic characteristics of delafloxacin."( Clinical and pharmacokinetic drug evaluation of delafloxacin for the treatment of acute bacterial skin and skin structure infections.
Bassetti, M; Cojutti, P; Pea, F; Pecori, D; Righi, E, 2017
)
0.46
" Blood and urine samples were collected, and pharmacokinetic parameters were calculated using noncompartmental methods."( Pharmacokinetics of Intravenous Delafloxacin in Patients With End-Stage Renal Disease.
Alcorn, H; Cammarata, SK; Hoover, R; Lawrence, L; Paulson, SK; Quintas, M, 2018
)
0.48

Bioavailability

ExcerptReferenceRelevance
" In addition, the absolute bioavailability (BA) of the 450-mg tablet formulation of delafloxacin was determined."( Safety, Tolerability, and Pharmacokinetic Properties of Intravenous Delafloxacin After Single and Multiple Doses in Healthy Volunteers.
Benedict, M; Cammarata, S; Hoover, R; Hunt, T; Lawrence, L; Paulson, SK; Sun, E, 2016
)
0.43
" The mean absolute bioavailability of delafloxacin was 58."( Safety, Tolerability, and Pharmacokinetic Properties of Intravenous Delafloxacin After Single and Multiple Doses in Healthy Volunteers.
Benedict, M; Cammarata, S; Hoover, R; Hunt, T; Lawrence, L; Paulson, SK; Sun, E, 2016
)
0.43
" The bioavailability is high (60-70%) and absorption is not affected by food intake, although further studies are required under clinically relevant conditions."( Clinical Pharmacokinetics and Pharmacodynamics of Delafloxacin.
Kiang, TK; Shiu, J; Ting, G, 2019
)
0.51
" Delafloxacin shows favorable pharmacological properties, with about 60% bioavailability after oral administration, only mild inhibition of cytochrome P450 3A, and no evidence of cardiac- or phototoxicity in healthy volunteers (tested against positive controls)."( Profile of a Novel Anionic Fluoroquinolone-Delafloxacin.
Tulkens, PM; Van Bambeke, F; Zinner, SH, 2019
)
0.51
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

ExcerptRelevanceReference
" Areas between the control growth and the time--kill curves (ABBC in single dose simulations and the sum of ABBCs determined after the first, second and third dosing in multiple dose simulations--ABBC(1+2+3)) were higher with ABT492 than levofloxacin."( ABT492 and levofloxacin: comparison of their pharmacodynamics and their abilities to prevent the selection of resistant Staphylococcus aureus in an in vitro dynamic model.
Arzamastsev, AP; Firsov, AA; Lubenko, IY; Portnoy, YA; Vostrov, SN; Zinner, SH, 2004
)
0.32
"5, 3, 4, 5, 6, 12, 18, and 24 h after dosing with delafloxacin at 300 mg intravenously (i."( A thorough QT study to evaluate the effects of therapeutic and supratherapeutic doses of delafloxacin on cardiac repolarization.
Benedict, MS; Cammarata, SK; Lawrence, LE; Litwin, JS; Sun, E; Thorn, MD, 2015
)
0.42
" Steady state was reached by day 3 of dosing with minimal accumulation of delafloxacin."( Single and Multiple Ascending-dose Studies of Oral Delafloxacin: Effects of Food, Sex, and Age.
Benedict, M; Cammarata, S; Hoover, R; Hunt, T; Lawrence, L; Paulson, SK; Sun, E, 2016
)
0.43
"Delafloxacin exhibits linear pharmacokinetic parameters that reached steady state after 3 days of daily oral dosing with minimal accumulation."( Single and Multiple Ascending-dose Studies of Oral Delafloxacin: Effects of Food, Sex, and Age.
Benedict, M; Cammarata, S; Hoover, R; Hunt, T; Lawrence, L; Paulson, SK; Sun, E, 2016
)
0.43
" The second study was a randomized, double-blind, placebo-controlled study of IV delafloxacin (300 mg) given as a single dose on day 1, followed by twice-daily dosing on days 2 through 14; 12 (8 active, 4 placebo) healthy volunteers were enrolled."( Safety, Tolerability, and Pharmacokinetic Properties of Intravenous Delafloxacin After Single and Multiple Doses in Healthy Volunteers.
Benedict, M; Cammarata, S; Hoover, R; Hunt, T; Lawrence, L; Paulson, SK; Sun, E, 2016
)
0.43
" A neutropenic murine lung infection model was utilized for all treatment studies, and drug dosing was by the subcutaneous route."( In Vivo Pharmacodynamic Target Assessment of Delafloxacin against Staphylococcus aureus, Streptococcus pneumoniae, and Klebsiella pneumoniae in a Murine Lung Infection Model.
Andes, DR; Lepak, AJ, 2016
)
0.43
"6 higher for subjects with ESRD compared to healthy subjects when dosed 1 hour before or 1 hour after hemodialysis, respectively."( Pharmacokinetics of Intravenous Delafloxacin in Patients With End-Stage Renal Disease.
Alcorn, H; Cammarata, SK; Hoover, R; Lawrence, L; Paulson, SK; Quintas, M, 2018
)
0.48
" Delafloxacin was dosed at 300 mg IV every 12 hours in Study 302; dosing in Study 303 was 300 mg IV every 12 hours for 3 days, with a mandatory, blinded switch to delafloxacin at 450 mg orally every 12 hours."( Analysis of Pooled Phase III Efficacy Data for Delafloxacin in Acute Bacterial Skin and Skin Structure Infections.
Cammarata, S; Giordano, PA; Pogue, JM, 2019
)
0.51
" Additional testing with alternative dosing regimens could be considered."( Efficacy and Safety of Single-Dose Oral Delafloxacin Compared With Intramuscular Ceftriaxone for Uncomplicated Gonorrhea Treatment: An Open-Label, Noninferiority, Phase 3, Multicenter, Randomized Study.
Cammarata, S; Golden, MR; Henry, E; Hook, EW; Nenninger, A; Swerdlow, J; Taylor, SN; Tseng, C; Workowski, KA, 2019
)
0.51
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (10)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
GVesicular stomatitis virusPotency16.59470.01238.964839.8107AID1645842
Interferon betaHomo sapiens (human)Potency16.59470.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency16.59470.01238.964839.8107AID1645842
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency16.59470.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency16.59470.01238.964839.8107AID1645842
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Cytochrome P450 1A2Homo sapiens (human)IC50 (µMol)50.00000.00011.774010.0000AID1723723
Cytochrome P450 3A4Homo sapiens (human)IC50 (µMol)50.00000.00011.753610.0000AID1723727
Cytochrome P450 2D6Homo sapiens (human)IC50 (µMol)50.00000.00002.015110.0000AID1723726
Cytochrome P450 2C9 Homo sapiens (human)IC50 (µMol)50.00000.00002.800510.0000AID1723725
Cytochrome P450 2C19Homo sapiens (human)IC50 (µMol)50.00000.00002.398310.0000AID1723724
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (87)

Processvia Protein(s)Taxonomy
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
positive regulation of T cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
adaptive immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-independentHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of T cell anergyHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
defense responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
detection of bacteriumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-12 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-6 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protection from natural killer cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
innate immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of dendritic cell differentiationHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class IbHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
steroid catabolic processCytochrome P450 1A2Homo sapiens (human)
porphyrin-containing compound metabolic processCytochrome P450 1A2Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 1A2Homo sapiens (human)
cholesterol metabolic processCytochrome P450 1A2Homo sapiens (human)
estrogen metabolic processCytochrome P450 1A2Homo sapiens (human)
toxin biosynthetic processCytochrome P450 1A2Homo sapiens (human)
post-embryonic developmentCytochrome P450 1A2Homo sapiens (human)
alkaloid metabolic processCytochrome P450 1A2Homo sapiens (human)
regulation of gene expressionCytochrome P450 1A2Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 1A2Homo sapiens (human)
dibenzo-p-dioxin metabolic processCytochrome P450 1A2Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 1A2Homo sapiens (human)
lung developmentCytochrome P450 1A2Homo sapiens (human)
methylationCytochrome P450 1A2Homo sapiens (human)
monocarboxylic acid metabolic processCytochrome P450 1A2Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 1A2Homo sapiens (human)
retinol metabolic processCytochrome P450 1A2Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 1A2Homo sapiens (human)
cellular respirationCytochrome P450 1A2Homo sapiens (human)
aflatoxin metabolic processCytochrome P450 1A2Homo sapiens (human)
hydrogen peroxide biosynthetic processCytochrome P450 1A2Homo sapiens (human)
oxidative demethylationCytochrome P450 1A2Homo sapiens (human)
cellular response to cadmium ionCytochrome P450 1A2Homo sapiens (human)
omega-hydroxylase P450 pathwayCytochrome P450 1A2Homo sapiens (human)
lipid hydroxylationCytochrome P450 3A4Homo sapiens (human)
lipid metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid catabolic processCytochrome P450 3A4Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid metabolic processCytochrome P450 3A4Homo sapiens (human)
cholesterol metabolic processCytochrome P450 3A4Homo sapiens (human)
androgen metabolic processCytochrome P450 3A4Homo sapiens (human)
estrogen metabolic processCytochrome P450 3A4Homo sapiens (human)
alkaloid catabolic processCytochrome P450 3A4Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 3A4Homo sapiens (human)
calcitriol biosynthetic process from calciolCytochrome P450 3A4Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D metabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D catabolic processCytochrome P450 3A4Homo sapiens (human)
retinol metabolic processCytochrome P450 3A4Homo sapiens (human)
retinoic acid metabolic processCytochrome P450 3A4Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 3A4Homo sapiens (human)
aflatoxin metabolic processCytochrome P450 3A4Homo sapiens (human)
oxidative demethylationCytochrome P450 3A4Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2D6Homo sapiens (human)
steroid metabolic processCytochrome P450 2D6Homo sapiens (human)
cholesterol metabolic processCytochrome P450 2D6Homo sapiens (human)
estrogen metabolic processCytochrome P450 2D6Homo sapiens (human)
coumarin metabolic processCytochrome P450 2D6Homo sapiens (human)
alkaloid metabolic processCytochrome P450 2D6Homo sapiens (human)
alkaloid catabolic processCytochrome P450 2D6Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2D6Homo sapiens (human)
isoquinoline alkaloid metabolic processCytochrome P450 2D6Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2D6Homo sapiens (human)
retinol metabolic processCytochrome P450 2D6Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 2D6Homo sapiens (human)
negative regulation of bindingCytochrome P450 2D6Homo sapiens (human)
oxidative demethylationCytochrome P450 2D6Homo sapiens (human)
negative regulation of cellular organofluorine metabolic processCytochrome P450 2D6Homo sapiens (human)
arachidonic acid metabolic processCytochrome P450 2D6Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2C9 Homo sapiens (human)
steroid metabolic processCytochrome P450 2C9 Homo sapiens (human)
cholesterol metabolic processCytochrome P450 2C9 Homo sapiens (human)
estrogen metabolic processCytochrome P450 2C9 Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2C9 Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 2C9 Homo sapiens (human)
urea metabolic processCytochrome P450 2C9 Homo sapiens (human)
monocarboxylic acid metabolic processCytochrome P450 2C9 Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2C9 Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 2C9 Homo sapiens (human)
amide metabolic processCytochrome P450 2C9 Homo sapiens (human)
icosanoid biosynthetic processCytochrome P450 2C9 Homo sapiens (human)
oxidative demethylationCytochrome P450 2C9 Homo sapiens (human)
omega-hydroxylase P450 pathwayCytochrome P450 2C9 Homo sapiens (human)
long-chain fatty acid metabolic processCytochrome P450 2C19Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2C19Homo sapiens (human)
steroid metabolic processCytochrome P450 2C19Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2C19Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 2C19Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2C19Homo sapiens (human)
omega-hydroxylase P450 pathwayCytochrome P450 2C19Homo sapiens (human)
inositol phosphate metabolic processInositol hexakisphosphate kinase 1Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
negative regulation of cold-induced thermogenesisInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (51)

Processvia Protein(s)Taxonomy
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
signaling receptor bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
peptide antigen bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein-folding chaperone bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
monooxygenase activityCytochrome P450 1A2Homo sapiens (human)
iron ion bindingCytochrome P450 1A2Homo sapiens (human)
protein bindingCytochrome P450 1A2Homo sapiens (human)
electron transfer activityCytochrome P450 1A2Homo sapiens (human)
oxidoreductase activityCytochrome P450 1A2Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 1A2Homo sapiens (human)
enzyme bindingCytochrome P450 1A2Homo sapiens (human)
heme bindingCytochrome P450 1A2Homo sapiens (human)
demethylase activityCytochrome P450 1A2Homo sapiens (human)
caffeine oxidase activityCytochrome P450 1A2Homo sapiens (human)
aromatase activityCytochrome P450 1A2Homo sapiens (human)
estrogen 16-alpha-hydroxylase activityCytochrome P450 1A2Homo sapiens (human)
estrogen 2-hydroxylase activityCytochrome P450 1A2Homo sapiens (human)
hydroperoxy icosatetraenoate dehydratase activityCytochrome P450 1A2Homo sapiens (human)
monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
steroid bindingCytochrome P450 3A4Homo sapiens (human)
iron ion bindingCytochrome P450 3A4Homo sapiens (human)
protein bindingCytochrome P450 3A4Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
retinoic acid 4-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
oxidoreductase activityCytochrome P450 3A4Homo sapiens (human)
oxygen bindingCytochrome P450 3A4Homo sapiens (human)
enzyme bindingCytochrome P450 3A4Homo sapiens (human)
heme bindingCytochrome P450 3A4Homo sapiens (human)
vitamin D3 25-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
caffeine oxidase activityCytochrome P450 3A4Homo sapiens (human)
quinine 3-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
testosterone 6-beta-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1-alpha,25-dihydroxyvitamin D3 23-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
aromatase activityCytochrome P450 3A4Homo sapiens (human)
vitamin D 24-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 16-alpha-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 2-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1,8-cineole 2-exo-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
monooxygenase activityCytochrome P450 2D6Homo sapiens (human)
iron ion bindingCytochrome P450 2D6Homo sapiens (human)
oxidoreductase activityCytochrome P450 2D6Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2D6Homo sapiens (human)
heme bindingCytochrome P450 2D6Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
iron ion bindingCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid 14,15-epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid 11,12-epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
oxidoreductase activityCytochrome P450 2C9 Homo sapiens (human)
(S)-limonene 6-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
(S)-limonene 7-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
caffeine oxidase activityCytochrome P450 2C9 Homo sapiens (human)
(R)-limonene 6-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
aromatase activityCytochrome P450 2C9 Homo sapiens (human)
heme bindingCytochrome P450 2C9 Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2C9 Homo sapiens (human)
monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
iron ion bindingCytochrome P450 2C19Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 2C19Homo sapiens (human)
oxidoreductase activityCytochrome P450 2C19Homo sapiens (human)
(S)-limonene 6-monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
(S)-limonene 7-monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
oxygen bindingCytochrome P450 2C19Homo sapiens (human)
enzyme bindingCytochrome P450 2C19Homo sapiens (human)
heme bindingCytochrome P450 2C19Homo sapiens (human)
(R)-limonene 6-monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
aromatase activityCytochrome P450 2C19Homo sapiens (human)
long-chain fatty acid omega-1 hydroxylase activityCytochrome P450 2C19Homo sapiens (human)
arachidonic acid epoxygenase activityCytochrome P450 2C19Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2C19Homo sapiens (human)
inositol-1,3,4,5,6-pentakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol heptakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
ATP bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 1-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 3-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (25)

Processvia Protein(s)Taxonomy
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
Golgi membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
endoplasmic reticulumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
Golgi apparatusHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
cell surfaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
ER to Golgi transport vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
secretory granule membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
phagocytic vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
early endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
recycling endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular exosomeHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
lumenal side of endoplasmic reticulum membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
MHC class I protein complexHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular spaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
external side of plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 1A2Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 1A2Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 1A2Homo sapiens (human)
cytoplasmCytochrome P450 3A4Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 3A4Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 3A4Homo sapiens (human)
mitochondrionCytochrome P450 2D6Homo sapiens (human)
endoplasmic reticulumCytochrome P450 2D6Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2D6Homo sapiens (human)
cytoplasmCytochrome P450 2D6Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2D6Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2C9 Homo sapiens (human)
plasma membraneCytochrome P450 2C9 Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C9 Homo sapiens (human)
cytoplasmCytochrome P450 2C9 Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C9 Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2C19Homo sapiens (human)
plasma membraneCytochrome P450 2C19Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C19Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C19Homo sapiens (human)
cytoplasmCytochrome P450 2C19Homo sapiens (human)
fibrillar centerInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
cytosolInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleusInositol hexakisphosphate kinase 1Homo sapiens (human)
cytoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (28)

Assay IDTitleYearJournalArticle
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1723719Antibacterial activity against Staphylococcus aureus ATCC 29213 assessed as reduction in bacterial growth by CLSI protocol based microdilution method2020Bioorganic & medicinal chemistry letters, 10-15, Volume: 30, Issue:20
Novel C-7 carbon substituted fourth generation fluoroquinolones targeting N. Gonorrhoeae infections.
AID1723730Distribution coefficient, logD of the compound at pH 7.42020Bioorganic & medicinal chemistry letters, 10-15, Volume: 30, Issue:20
Novel C-7 carbon substituted fourth generation fluoroquinolones targeting N. Gonorrhoeae infections.
AID1723724Inhibition of CYP2C19 (unknown origin)2020Bioorganic & medicinal chemistry letters, 10-15, Volume: 30, Issue:20
Novel C-7 carbon substituted fourth generation fluoroquinolones targeting N. Gonorrhoeae infections.
AID1723732Oral bioavailability in human at 450 mg measured every 12 hrs2020Bioorganic & medicinal chemistry letters, 10-15, Volume: 30, Issue:20
Novel C-7 carbon substituted fourth generation fluoroquinolones targeting N. Gonorrhoeae infections.
AID1723729Kinetic solubility of the compound2020Bioorganic & medicinal chemistry letters, 10-15, Volume: 30, Issue:20
Novel C-7 carbon substituted fourth generation fluoroquinolones targeting N. Gonorrhoeae infections.
AID1723731Acid dissociation constant, pKa of the compound2020Bioorganic & medicinal chemistry letters, 10-15, Volume: 30, Issue:20
Novel C-7 carbon substituted fourth generation fluoroquinolones targeting N. Gonorrhoeae infections.
AID1723727Inhibition of CYP3A4 (unknown origin)2020Bioorganic & medicinal chemistry letters, 10-15, Volume: 30, Issue:20
Novel C-7 carbon substituted fourth generation fluoroquinolones targeting N. Gonorrhoeae infections.
AID1723718Antibacterial activity against Escherichia coli ATCC 25922 assessed as reduction in bacterial growth by CLSI protocol based microdilution method2020Bioorganic & medicinal chemistry letters, 10-15, Volume: 30, Issue:20
Novel C-7 carbon substituted fourth generation fluoroquinolones targeting N. Gonorrhoeae infections.
AID1723735Antibacterial activity against Neisseria gonorrhoeae assessed as reduction in bacterial growth2020Bioorganic & medicinal chemistry letters, 10-15, Volume: 30, Issue:20
Novel C-7 carbon substituted fourth generation fluoroquinolones targeting N. Gonorrhoeae infections.
AID1723737Inhibition of human ERG up to 185 uM2020Bioorganic & medicinal chemistry letters, 10-15, Volume: 30, Issue:20
Novel C-7 carbon substituted fourth generation fluoroquinolones targeting N. Gonorrhoeae infections.
AID1723722Intrinsic clearance in human hepatocytes assessed per 10^6 cells2020Bioorganic & medicinal chemistry letters, 10-15, Volume: 30, Issue:20
Novel C-7 carbon substituted fourth generation fluoroquinolones targeting N. Gonorrhoeae infections.
AID1723728Protein binding in human plasma assessed as free fraction2020Bioorganic & medicinal chemistry letters, 10-15, Volume: 30, Issue:20
Novel C-7 carbon substituted fourth generation fluoroquinolones targeting N. Gonorrhoeae infections.
AID1723714Antibacterial activity against Neisseria gonorrhoeae ATCC 49226 assessed as reduction in bacterial growth by CLSI protocol based microdilution method2020Bioorganic & medicinal chemistry letters, 10-15, Volume: 30, Issue:20
Novel C-7 carbon substituted fourth generation fluoroquinolones targeting N. Gonorrhoeae infections.
AID1723738Inhibition of human ERG at 100 uM relative to control2020Bioorganic & medicinal chemistry letters, 10-15, Volume: 30, Issue:20
Novel C-7 carbon substituted fourth generation fluoroquinolones targeting N. Gonorrhoeae infections.
AID1723721Intrinsic clearance in human liver microsomes2020Bioorganic & medicinal chemistry letters, 10-15, Volume: 30, Issue:20
Novel C-7 carbon substituted fourth generation fluoroquinolones targeting N. Gonorrhoeae infections.
AID1723723Inhibition of CYP1A2 (unknown origin)2020Bioorganic & medicinal chemistry letters, 10-15, Volume: 30, Issue:20
Novel C-7 carbon substituted fourth generation fluoroquinolones targeting N. Gonorrhoeae infections.
AID1723720Antibacterial activity against Enterococcus faecalis ATCC 29212 assessed as reduction in bacterial growth by CLSI protocol based microdilution method2020Bioorganic & medicinal chemistry letters, 10-15, Volume: 30, Issue:20
Novel C-7 carbon substituted fourth generation fluoroquinolones targeting N. Gonorrhoeae infections.
AID1723725Inhibition of CYP2C9 (unknown origin)2020Bioorganic & medicinal chemistry letters, 10-15, Volume: 30, Issue:20
Novel C-7 carbon substituted fourth generation fluoroquinolones targeting N. Gonorrhoeae infections.
AID1723715Antibacterial activity against fluoroquinolone-resistant Neisseria gonorrhoeae WHO L harboring multiple point mutations at DNA gyrase and topoisomerase IV and porB1b mutation assessed as reduction in bacterial growth by CLSI protocol based microdilution m2020Bioorganic & medicinal chemistry letters, 10-15, Volume: 30, Issue:20
Novel C-7 carbon substituted fourth generation fluoroquinolones targeting N. Gonorrhoeae infections.
AID1723716Antibacterial activity against Acinetobacter baumannii ATCC 19606 assessed as reduction in bacterial growth by CLSI protocol based microdilution method2020Bioorganic & medicinal chemistry letters, 10-15, Volume: 30, Issue:20
Novel C-7 carbon substituted fourth generation fluoroquinolones targeting N. Gonorrhoeae infections.
AID1723717Antibacterial activity against Klebsiella pneumoniae ATCC 700603 assessed as reduction in bacterial growth by CLSI protocol based microdilution method2020Bioorganic & medicinal chemistry letters, 10-15, Volume: 30, Issue:20
Novel C-7 carbon substituted fourth generation fluoroquinolones targeting N. Gonorrhoeae infections.
AID1723726Inhibition of CYP2D6 (unknown origin)2020Bioorganic & medicinal chemistry letters, 10-15, Volume: 30, Issue:20
Novel C-7 carbon substituted fourth generation fluoroquinolones targeting N. Gonorrhoeae infections.
AID1723713Antibacterial activity against Pseudomonas aeruginosa PAO1 assessed as reduction in bacterial growth by CLSI protocol based microdilution method2020Bioorganic & medicinal chemistry letters, 10-15, Volume: 30, Issue:20
Novel C-7 carbon substituted fourth generation fluoroquinolones targeting N. Gonorrhoeae infections.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (92)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's14 (15.22)29.6817
2010's43 (46.74)24.3611
2020's35 (38.04)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 16.38

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

MetricThis Compound (vs All)
Research Demand Index16.38 (24.57)
Research Supply Index4.71 (2.92)
Research Growth Index5.90 (4.65)
Search Engine Demand Index10.37 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (16.38)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials17 (18.28%)5.53%
Reviews21 (22.58%)6.00%
Case Studies1 (1.08%)4.05%
Observational0 (0.00%)0.25%
Other54 (58.06%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]