Page last updated: 2024-07-31 17:58:35

ul-fs 49

Description

Cross-References

ID SourceID
PubMed CID3045335
CHEMBL ID543767
SCHEMBL ID1588590
MeSH IDM0128279

Synonyms (44)

Synonym
ul-fs-49
zatebradine hydrochloride
zatebradine hydrochloride, >=98% (hplc), powder
NCGC00092334-01
ul-fs 49
2h-3-benzazepin-2-one, 3-(3-((2-(3,4-dimethoxyphenyl)ethyl)methylamino)propyl)-1,3,4,5-tetrahydro-7,8-dimethoxy-, monohydrochloride
CHEMBL543767
3-[3-[2-(3,4-dimethoxyphenyl)ethyl-methylamino]propyl]-7,8-dimethoxy-2,5-dihydro-1h-3-benzazepin-4-one hydrochloride
zatebradine hcl
91940-87-3
wjb7dyv16a ,
unii-wjb7dyv16a
dtxsid6045745 ,
cas-91940-87-3
dtxcid4025745
tox21_111195
7,8-dimethoxy-3-[3-[-n-[2-(3,4 dimethoxyphenyl)ethyl]-n-methylamino]propyl]-1,3,4,5-tetrahydro-2h-3-benzazepin-2-one hydrochloride
3-[3-[[2-(3,4-dimethoxyphenyl)ethyl]methylamino]propyl]-1,3,4,5-tetrahydro-7,8-dimethoxy-2h-3-benzazepin-2-one hydrochloride
3-(3-((2-(3,4-dimethoxyphenyl)ethyl)methylamino)propyl)-1,3,4,5-tetrahydro-7,8-dimethoxy-2h-3-benzazepin-2-one, hydrochloride
zatebradine hydrochloride [mi]
2h-3-benzazepin-2-one, 3-(3-((2-(3,4-dimethoxyphenyl)ethyl)methylamino)propyl)-1,3,4,5-tetrahydro-7,8-dimethoxy-, hydrochloride (1:1)
ulfs-49cl
SCHEMBL1588590
tox21_111195_1
NCGC00092334-02
ZRNKXJHEQKMWCH-UHFFFAOYSA-N
1-[7,8-dimethoxy-1,3,4,5-tetrahydro-2h-3-benzazepin-2-on-3-yl]-3-[n-methyl-n-(2-{3,4-dimethoxy-phenyl}-ethyl)-amino]-propane hydrochloride
CS-3619
3-(3-{[2-(3,4-dimethoxy-phenyl)-ethyl]-methyl-amino}-propyl)-7,8-dimethoxy-1,3,4,5-tetrahydro-benzo[d]azepin-2-one hydrochloride
zatebradine (hydrochloride)
HY-13422
AKOS024456987
A922768
ul-fs-49cl
FT-0734393
ul-fs-49;ul-fs-49cl
zatebradine hydrochloride; ul-fs49; ul fs49; ulfs49;ul-fs-49; ul-fs-49cl
BCP11021
Q27292671
3-[3-[[2-(3,4-dimethoxyphenyl)ethyl]methylamino]propyl]-1,3,4,5-tetrahydro-7,8-dimethoxy-2h-3-benzazepin-2-one hydrochlorid
MS-29159
3-[3-[2-(3,4-dimethoxyphenyl)ethyl-methylamino]propyl]-7,8-dimethoxy-2,5-dihydro-1h-3-benzazepin-4-one;hydrochloride
zatebradinehydrochloride
E98759

Protein Targets (24)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)
15-lipoxygenase, partialHomo sapiens (human)Potency0.0251AID887
GLI family zinc finger 3Homo sapiens (human)Potency25.6358AID1259369; AID1259392
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency32.2774AID1159552; AID1159553; AID1159555
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency33.4889AID743222
activating transcription factor 6Homo sapiens (human)Potency0.0054AID1159516
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency7.9433AID588834
heat shock protein beta-1Homo sapiens (human)Potency33.4889AID743210
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency12.5893AID884; AID885
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency12.5893AID885
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency12.5893AID885
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency12.5893AID885
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency12.5893AID885
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency12.5893AID885
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency12.5893AID885
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency12.5893AID885
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency12.5893AID885
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency12.5893AID885
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency12.5893AID885
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency12.5893AID885
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency12.5893AID885
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency12.5893AID885
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency12.5893AID885
GABA theta subunitRattus norvegicus (Norway rat)Potency12.5893AID885
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency12.5893AID885

Bioassays (44)

Assay IDTitleYearJournalArticle
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
ISSN: 2472-5560
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
ISSN: 1091-6490
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
ISSN: 2211-1247
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
ISSN: 1521-0111
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
ISSN: 1521-0111
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID167565Evaluated in vitro for the effect on K+ induced aortic contraction in isolated aortic strips of rabbit1990Journal of medicinal chemistry, May, Volume: 33, Issue:5
ISSN: 0022-2623
Specific bradycardic agents. 1. Chemistry, pharmacology, and structure-activity relationships of substituted benzazepinones, a-new class of compounds exerting antiischemic properties.
AID47774Evaluated in vivo for bradycardic activity in anesthetized cat as a measure of % decrease of heart rate after 1 mg/Kg intravenous administration of the compound.1990Journal of medicinal chemistry, May, Volume: 33, Issue:5
ISSN: 0022-2623
Specific bradycardic agents. 1. Chemistry, pharmacology, and structure-activity relationships of substituted benzazepinones, a-new class of compounds exerting antiischemic properties.
AID172519In vivo effect on mean blood pressure of anesthetized rats following 3 mg/kg i.v.2003Journal of medicinal chemistry, Oct-23, Volume: 46, Issue:22
ISSN: 0022-2623
Synthesis and pharmacological evaluation of 1-oxo-2-(3-piperidyl)-1,2,3,4- tetrahydroisoquinolines and related analogues as a new class of specific bradycardic agents possessing I(f) channel inhibitory activity.
AID172393In vivo effect on heart rate of anesthetized rats following 3 mg/kg i.v.2003Journal of medicinal chemistry, Oct-23, Volume: 46, Issue:22
ISSN: 0022-2623
Synthesis and pharmacological evaluation of 1-oxo-2-(3-piperidyl)-1,2,3,4- tetrahydroisoquinolines and related analogues as a new class of specific bradycardic agents possessing I(f) channel inhibitory activity.
AID231902Ratio between the EC30 values of atrial contractility and atrial rate1990Journal of medicinal chemistry, May, Volume: 33, Issue:5
ISSN: 0022-2623
Specific bradycardic agents. 1. Chemistry, pharmacology, and structure-activity relationships of substituted benzazepinones, a-new class of compounds exerting antiischemic properties.
AID75924In vitro bradycardiac activity on isolated right atrium of guinea pig.2003Journal of medicinal chemistry, Oct-23, Volume: 46, Issue:22
ISSN: 0022-2623
Synthesis and pharmacological evaluation of 1-oxo-2-(3-piperidyl)-1,2,3,4- tetrahydroisoquinolines and related analogues as a new class of specific bradycardic agents possessing I(f) channel inhibitory activity.
AID80745Evaluated in vitro for its effect on spontaneous atrial contractility in isolated guinea pig atria1990Journal of medicinal chemistry, May, Volume: 33, Issue:5
ISSN: 0022-2623
Specific bradycardic agents. 1. Chemistry, pharmacology, and structure-activity relationships of substituted benzazepinones, a-new class of compounds exerting antiischemic properties.
AID80746Evaluated in vitro for the effect on spontaneous atrial rate in isolated guinea pig atria1990Journal of medicinal chemistry, May, Volume: 33, Issue:5
ISSN: 0022-2623
Specific bradycardic agents. 1. Chemistry, pharmacology, and structure-activity relationships of substituted benzazepinones, a-new class of compounds exerting antiischemic properties.
AID231901Ratio between the EC30 values of aortic contracture and atrial rate1990Journal of medicinal chemistry, May, Volume: 33, Issue:5
ISSN: 0022-2623
Specific bradycardic agents. 1. Chemistry, pharmacology, and structure-activity relationships of substituted benzazepinones, a-new class of compounds exerting antiischemic properties.
AID176122Bradycardic activity measured as a percentage decrease of heart rate after 5 mg/kg intravenous administration in anesthetized rats1990Journal of medicinal chemistry, May, Volume: 33, Issue:5
ISSN: 0022-2623
Specific bradycardic agents. 1. Chemistry, pharmacology, and structure-activity relationships of substituted benzazepinones, a-new class of compounds exerting antiischemic properties.
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
ISSN: 1095-9203
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
ISSN: 1083-351X
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173ISSN: 1872-9096A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression2022The Journal of biological chemistry, 08, Volume: 298, Issue:8
ISSN: 1083-351X
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
ISSN: 1554-8937
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
ISSN: 1083-351X
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173ISSN: 1872-9096A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845Primary qHTS for Inhibitors of ATXN expression2022The Journal of biological chemistry, 08, Volume: 298, Issue:8
ISSN: 1083-351X
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173ISSN: 1872-9096A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.

Research

Studies (12)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's1 (8.33)18.2507
2000's1 (8.33)29.6817
2010's4 (33.33)24.3611
2020's6 (50.00)2.80

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%
Other12 (100.00%)84.16%
SubstanceStudiesClassesRolesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
nifedipineC-nitro compound;
dihydropyridine;
methyl ester
calcium channel blocker;
human metabolite;
tocolytic agent;
vasodilator agent
1990199034.0high001000
diltiazem5-[2-(dimethylamino)ethyl]-2-(4-methoxyphenyl)-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepin-3-yl acetateantihypertensive agent;
calcium channel blocker;
vasodilator agent
1990199034.0high001000
lekoptin2-(3,4-dimethoxyphenyl)-5-{[2-(3,4-dimethoxyphenyl)ethyl](methyl)amino}-2-(propan-2-yl)pentanenitrile1990199034.0high001000
ConditionIndicatedStudiesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
Congenital Zika Syndrome0202020204.0medium000010
Coronary Disease01990199034.0medium001000
Coronary Heart Disease01990199034.0medium001000
Disease Models, Animal0202020204.0medium000010
Zika Virus Infection0202020204.0medium000010

Bioavailability (2)

ArticleYear
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Molecular pharmacology, , Volume: 96, Issue:5
2019
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
The Journal of biological chemistry, , 11-15, Volume: 294, Issue:46
2019