Page last updated: 2024-11-13

(5-bromo-3-pyridinyl)-[4-(1-pyrrolidinyl)-1-piperidinyl]methanone

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

(5-bromo-3-pyridinyl)-[4-(1-pyrrolidinyl)-1-piperidinyl]methanone, also known as **GW405833**, is a selective antagonist of the **neuronal nicotinic acetylcholine receptor (nAChR)**.

Here's why it's important for research:

**1. Understanding nAChR Function:**

* **nAChRs are crucial for a variety of physiological processes:** including learning, memory, muscle contraction, and pain perception.
* **GW405833 provides a valuable tool for studying specific nAChR subtypes:** by blocking their activity, researchers can understand their individual roles in these processes.

**2. Drug Development:**

* **GW405833 is a lead compound for the development of new drugs targeting nAChRs:** These drugs could potentially treat a range of disorders, including:
* **Alzheimer's disease:** by improving cognitive function.
* **Schizophrenia:** by modulating neuronal signaling.
* **Pain:** by reducing pain perception.
* **Nicotine addiction:** by reducing the rewarding effects of nicotine.

**3. Studying Neurobiology:**

* **GW405833 is used in animal models to study the effects of nAChR inhibition:** This research contributes to our understanding of brain function and can inform the development of new therapeutic strategies for various neurological conditions.

**4. Pharmacology Research:**

* **GW405833 is a powerful tool for pharmacologists:** It allows them to investigate the mechanisms of action of different drugs and to identify potential drug targets.

**Important Note:**

While GW405833 holds great promise for research and drug development, its use is currently limited to laboratory settings. It is not approved for clinical use in humans.

**In summary, (5-bromo-3-pyridinyl)-[4-(1-pyrrolidinyl)-1-piperidinyl]methanone is a valuable research tool that provides insights into nAChR function, facilitates drug development, and contributes to our understanding of neurobiology.**

Cross-References

ID SourceID
PubMed CID46931242
CHEMBL ID1235119
CHEBI ID95085
SCHEMBL ID23682640

Synonyms (41)

Synonym
CHEMBL1235119 ,
p8h ,
3-bromo-5-[(4-pyrrolidin-1-ylpiperidin-1-yl)carbonyl]pyridine
bdbm50341828
5-bromo-n-(4-(pyrrolidinyl)piperidinyl)nicotinamide
AKOS010495586
NCGC00347957-01
S7373
1314241-44-5
unc669
HY-15839
unc 669
smr004701326
MLS006010250
c15h20brn3o
unc-669
(5-bromopyridin-3-yl)(4-(pyrrolidin-1-yl)piperidin-1-yl)methanone
unc0669
EX-A257
CHEBI:95085
HMS3653O18
mfcd26936345
3-bromo-5-[4-(pyrrolidin-1-yl)piperidine-1-carbonyl]pyridine
NCGC00347957-09
SW220043-1
(5-bromopyridin-3-yl)[4-(pyrrolidin-1-yl)piperidin-1-yl]methanone
FT-0739051
Q27166853
(5-bromo-3-pyridinyl)-[4-(1-pyrrolidinyl)-1-piperidinyl]methanone
unc 669;unc-669
BCP27815
SB19336
(5-bromopyridin-3-yl)-(4-pyrrolidin-1-ylpiperidin-1-yl)methanone
HMS3426C15
CCG-267893
A935152
(5-bromo-3-pyridinyl)[4-(1-pyrrolidinyl)-1-piperidinyl]methanone
AS-55925
SCHEMBL23682640
DTXSID301025591
AC-35780

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
"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
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (2)

ClassDescription
aromatic carboxylic acidAny carboxylic acid in which the carboxy group is directly bonded to an aromatic ring.
pyridinemonocarboxylic acidA monocarboxylic acid in which the carboxy group is attached to a pyridine (or substituted pyridine) ring.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (12)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Fumarate hydrataseHomo sapiens (human)Potency0.18650.00308.794948.0869AID1347053
polyproteinZika virusPotency0.18650.00308.794948.0869AID1347053
[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)
Lysine-specific demethylase 5AHomo sapiens (human)IC50 (µMol)20.00000.13002.374710.0000AID1077871; AID771611
MBT domain-containing protein 1Homo sapiens (human)IC50 (µMol)155.00009.00009.00009.0000AID1077875; AID771615
Lethal(3)malignant brain tumor-like protein 3Homo sapiens (human)IC50 (µMol)11.40000.02401.40964.7000AID1077877; AID593469; AID771620; AID771621
Lethal(3)malignant brain tumor-like protein 1Homo sapiens (human)IC50 (µMol)10.40000.09804.29968.9000AID1077876; AID593468; AID771619
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Lethal(3)malignant brain tumor-like protein 1Homo sapiens (human)Kd7.50005.00008.133310.0000AID593463; AID593545
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (52)

Processvia Protein(s)Taxonomy
negative regulation of transcription by RNA polymerase IIChromobox protein homolog 7Homo sapiens (human)
chromatin organizationChromobox protein homolog 7Homo sapiens (human)
negative regulation of transcription by RNA polymerase IILysine-specific demethylase 5AHomo sapiens (human)
circadian regulation of gene expressionLysine-specific demethylase 5AHomo sapiens (human)
positive regulation of DNA-templated transcriptionLysine-specific demethylase 5AHomo sapiens (human)
regulation of DNA-binding transcription factor activityLysine-specific demethylase 5AHomo sapiens (human)
facultative heterochromatin formationLysine-specific demethylase 5AHomo sapiens (human)
regulation of DNA-templated transcriptionLysine-specific demethylase 5AHomo sapiens (human)
chromatin remodelingLysine-specific demethylase 5AHomo sapiens (human)
double-strand break repair via homologous recombinationMBT domain-containing protein 1Homo sapiens (human)
chromatin organizationMBT domain-containing protein 1Homo sapiens (human)
regulation of apoptotic processMBT domain-containing protein 1Homo sapiens (human)
positive regulation of DNA-templated transcriptionMBT domain-containing protein 1Homo sapiens (human)
embryonic skeletal system developmentMBT domain-containing protein 1Homo sapiens (human)
regulation of cell cycleMBT domain-containing protein 1Homo sapiens (human)
positive regulation of double-strand break repair via homologous recombinationMBT domain-containing protein 1Homo sapiens (human)
regulation of double-strand break repairMBT domain-containing protein 1Homo sapiens (human)
negative regulation of DNA-templated transcriptionMBT domain-containing protein 1Homo sapiens (human)
DNA damage responseTP53-binding protein 1Homo sapiens (human)
double-strand break repair via nonhomologous end joiningTP53-binding protein 1Homo sapiens (human)
chromatin organizationTP53-binding protein 1Homo sapiens (human)
DNA damage responseTP53-binding protein 1Homo sapiens (human)
positive regulation of isotype switchingTP53-binding protein 1Homo sapiens (human)
positive regulation of DNA-templated transcriptionTP53-binding protein 1Homo sapiens (human)
positive regulation of transcription by RNA polymerase IITP53-binding protein 1Homo sapiens (human)
positive regulation of DNA-binding transcription factor activityTP53-binding protein 1Homo sapiens (human)
protein homooligomerizationTP53-binding protein 1Homo sapiens (human)
cellular response to X-rayTP53-binding protein 1Homo sapiens (human)
double-strand break repair via classical nonhomologous end joiningTP53-binding protein 1Homo sapiens (human)
protein localization to site of double-strand breakTP53-binding protein 1Homo sapiens (human)
negative regulation of double-strand break repair via homologous recombinationTP53-binding protein 1Homo sapiens (human)
DNA damage checkpoint signalingTP53-binding protein 1Homo sapiens (human)
chromatin organizationLethal(3)malignant brain tumor-like protein 4Homo sapiens (human)
negative regulation of DNA-templated transcriptionLethal(3)malignant brain tumor-like protein 4Homo sapiens (human)
chromatin organizationLethal(3)malignant brain tumor-like protein 3Homo sapiens (human)
macrophage differentiationLethal(3)malignant brain tumor-like protein 3Homo sapiens (human)
granulocyte differentiationLethal(3)malignant brain tumor-like protein 3Homo sapiens (human)
erythrocyte maturationLethal(3)malignant brain tumor-like protein 3Homo sapiens (human)
negative regulation of DNA-templated transcriptionLethal(3)malignant brain tumor-like protein 3Homo sapiens (human)
regulation of DNA methylation-dependent heterochromatin formationLethal(3)malignant brain tumor-like protein 3Homo sapiens (human)
positive regulation of ubiquitin-dependent protein catabolic processLethal(3)malignant brain tumor-like protein 3Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIE3 ubiquitin-protein ligase UHRF1Homo sapiens (human)
double-strand break repair via homologous recombinationE3 ubiquitin-protein ligase UHRF1Homo sapiens (human)
ubiquitin-dependent protein catabolic processE3 ubiquitin-protein ligase UHRF1Homo sapiens (human)
DNA damage responseE3 ubiquitin-protein ligase UHRF1Homo sapiens (human)
heterochromatin formationE3 ubiquitin-protein ligase UHRF1Homo sapiens (human)
homologous recombinationE3 ubiquitin-protein ligase UHRF1Homo sapiens (human)
epigenetic regulation of gene expressionE3 ubiquitin-protein ligase UHRF1Homo sapiens (human)
negative regulation of gene expression via chromosomal CpG island methylationE3 ubiquitin-protein ligase UHRF1Homo sapiens (human)
positive regulation of transcription by RNA polymerase IIE3 ubiquitin-protein ligase UHRF1Homo sapiens (human)
regulation of epithelial cell proliferationE3 ubiquitin-protein ligase UHRF1Homo sapiens (human)
positive regulation of protein metabolic processE3 ubiquitin-protein ligase UHRF1Homo sapiens (human)
protein autoubiquitinationE3 ubiquitin-protein ligase UHRF1Homo sapiens (human)
mitotic spindle assemblyE3 ubiquitin-protein ligase UHRF1Homo sapiens (human)
positive regulation of DNA topoisomerase (ATP-hydrolyzing) activityE3 ubiquitin-protein ligase UHRF1Homo sapiens (human)
protein ubiquitinationE3 ubiquitin-protein ligase UHRF1Homo sapiens (human)
autophagyPHD finger protein 23Homo sapiens (human)
positive regulation of protein ubiquitinationPHD finger protein 23Homo sapiens (human)
negative regulation of autophagosome maturationPHD finger protein 23Homo sapiens (human)
negative regulation of autophagosome assemblyPHD finger protein 23Homo sapiens (human)
chromatin organizationScm-like with four MBT domains protein 1Homo sapiens (human)
spermatogenesisScm-like with four MBT domains protein 1Homo sapiens (human)
cell differentiationScm-like with four MBT domains protein 1Homo sapiens (human)
negative regulation of DNA-templated transcriptionScm-like with four MBT domains protein 1Homo sapiens (human)
negative regulation of muscle organ developmentScm-like with four MBT domains protein 1Homo sapiens (human)
chromatin organizationLethal(3)malignant brain tumor-like protein 1Homo sapiens (human)
regulation of mitotic nuclear divisionLethal(3)malignant brain tumor-like protein 1Homo sapiens (human)
hemopoiesisLethal(3)malignant brain tumor-like protein 1Homo sapiens (human)
heterochromatin formationLethal(3)malignant brain tumor-like protein 1Homo sapiens (human)
regulation of megakaryocyte differentiationLethal(3)malignant brain tumor-like protein 1Homo sapiens (human)
negative regulation of DNA-templated transcriptionLethal(3)malignant brain tumor-like protein 1Homo sapiens (human)
regulation of cell cycleLethal(3)malignant brain tumor-like protein 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (35)

Processvia Protein(s)Taxonomy
protein bindingChromobox protein homolog 7Homo sapiens (human)
transcription cis-regulatory region bindingLysine-specific demethylase 5AHomo sapiens (human)
DNA bindingLysine-specific demethylase 5AHomo sapiens (human)
transcription coactivator activityLysine-specific demethylase 5AHomo sapiens (human)
enzyme inhibitor activityLysine-specific demethylase 5AHomo sapiens (human)
protein bindingLysine-specific demethylase 5AHomo sapiens (human)
zinc ion bindingLysine-specific demethylase 5AHomo sapiens (human)
chromatin DNA bindingLysine-specific demethylase 5AHomo sapiens (human)
histone demethylase activityLysine-specific demethylase 5AHomo sapiens (human)
histone H3K4me/H3K4me2/H3K4me3 demethylase activityLysine-specific demethylase 5AHomo sapiens (human)
methylated histone bindingLysine-specific demethylase 5AHomo sapiens (human)
histone bindingLysine-specific demethylase 5AHomo sapiens (human)
protein bindingMBT domain-containing protein 1Homo sapiens (human)
zinc ion bindingMBT domain-containing protein 1Homo sapiens (human)
methylated histone bindingMBT domain-containing protein 1Homo sapiens (human)
NuA4 histone acetyltransferase complex bindingMBT domain-containing protein 1Homo sapiens (human)
chromatin bindingMBT domain-containing protein 1Homo sapiens (human)
p53 bindingTP53-binding protein 1Homo sapiens (human)
damaged DNA bindingTP53-binding protein 1Homo sapiens (human)
transcription coregulator activityTP53-binding protein 1Homo sapiens (human)
protein bindingTP53-binding protein 1Homo sapiens (human)
methylated histone bindingTP53-binding protein 1Homo sapiens (human)
telomeric DNA bindingTP53-binding protein 1Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingTP53-binding protein 1Homo sapiens (human)
ubiquitin-modified histone reader activityTP53-binding protein 1Homo sapiens (human)
histone reader activityTP53-binding protein 1Homo sapiens (human)
histone bindingTP53-binding protein 1Homo sapiens (human)
protein bindingLethal(3)malignant brain tumor-like protein 4Homo sapiens (human)
zinc ion bindingLethal(3)malignant brain tumor-like protein 4Homo sapiens (human)
histone bindingLethal(3)malignant brain tumor-like protein 4Homo sapiens (human)
chromatin bindingLethal(3)malignant brain tumor-like protein 4Homo sapiens (human)
chromatin bindingLethal(3)malignant brain tumor-like protein 3Homo sapiens (human)
protein bindingLethal(3)malignant brain tumor-like protein 3Homo sapiens (human)
zinc ion bindingLethal(3)malignant brain tumor-like protein 3Homo sapiens (human)
identical protein bindingLethal(3)malignant brain tumor-like protein 3Homo sapiens (human)
methylation-dependent protein bindingLethal(3)malignant brain tumor-like protein 3Homo sapiens (human)
histone bindingLethal(3)malignant brain tumor-like protein 3Homo sapiens (human)
cis-regulatory region sequence-specific DNA bindingE3 ubiquitin-protein ligase UHRF1Homo sapiens (human)
nucleic acid bindingE3 ubiquitin-protein ligase UHRF1Homo sapiens (human)
ubiquitin-protein transferase activityE3 ubiquitin-protein ligase UHRF1Homo sapiens (human)
protein bindingE3 ubiquitin-protein ligase UHRF1Homo sapiens (human)
zinc ion bindingE3 ubiquitin-protein ligase UHRF1Homo sapiens (human)
methyl-CpG bindingE3 ubiquitin-protein ligase UHRF1Homo sapiens (human)
methylated histone bindingE3 ubiquitin-protein ligase UHRF1Homo sapiens (human)
histone bindingE3 ubiquitin-protein ligase UHRF1Homo sapiens (human)
identical protein bindingE3 ubiquitin-protein ligase UHRF1Homo sapiens (human)
hemi-methylated DNA-bindingE3 ubiquitin-protein ligase UHRF1Homo sapiens (human)
ubiquitin protein ligase activityE3 ubiquitin-protein ligase UHRF1Homo sapiens (human)
H3K9me3 modified histone bindingE3 ubiquitin-protein ligase UHRF1Homo sapiens (human)
DNA damage sensor activityE3 ubiquitin-protein ligase UHRF1Homo sapiens (human)
histone H3 ubiquitin ligase activityE3 ubiquitin-protein ligase UHRF1Homo sapiens (human)
protein bindingPHD finger protein 23Homo sapiens (human)
metal ion bindingPHD finger protein 23Homo sapiens (human)
transcription corepressor activityScm-like with four MBT domains protein 1Homo sapiens (human)
protein bindingScm-like with four MBT domains protein 1Homo sapiens (human)
histone bindingScm-like with four MBT domains protein 1Homo sapiens (human)
chromatin bindingScm-like with four MBT domains protein 1Homo sapiens (human)
chromatin bindingLethal(3)malignant brain tumor-like protein 1Homo sapiens (human)
protein bindingLethal(3)malignant brain tumor-like protein 1Homo sapiens (human)
zinc ion bindingLethal(3)malignant brain tumor-like protein 1Homo sapiens (human)
nucleosome bindingLethal(3)malignant brain tumor-like protein 1Homo sapiens (human)
SAM domain bindingLethal(3)malignant brain tumor-like protein 1Homo sapiens (human)
methylated histone bindingLethal(3)malignant brain tumor-like protein 1Homo sapiens (human)
histone bindingLethal(3)malignant brain tumor-like protein 1Homo sapiens (human)
identical protein bindingLethal(3)malignant brain tumor-like protein 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (22)

Processvia Protein(s)Taxonomy
nucleusChromobox protein homolog 7Homo sapiens (human)
nucleoplasmChromobox protein homolog 7Homo sapiens (human)
cytosolChromobox protein homolog 7Homo sapiens (human)
chromatinChromobox protein homolog 7Homo sapiens (human)
PcG protein complexChromobox protein homolog 7Homo sapiens (human)
PRC1 complexChromobox protein homolog 7Homo sapiens (human)
nucleusLysine-specific demethylase 5AHomo sapiens (human)
nucleoplasmLysine-specific demethylase 5AHomo sapiens (human)
nucleolusLysine-specific demethylase 5AHomo sapiens (human)
nucleusLysine-specific demethylase 5AHomo sapiens (human)
chromatinLysine-specific demethylase 5AHomo sapiens (human)
site of double-strand breakMBT domain-containing protein 1Homo sapiens (human)
nucleosomeMBT domain-containing protein 1Homo sapiens (human)
NuA4 histone acetyltransferase complexMBT domain-containing protein 1Homo sapiens (human)
nucleusMBT domain-containing protein 1Homo sapiens (human)
chromosome, telomeric regionTP53-binding protein 1Homo sapiens (human)
site of double-strand breakTP53-binding protein 1Homo sapiens (human)
kinetochoreTP53-binding protein 1Homo sapiens (human)
nucleusTP53-binding protein 1Homo sapiens (human)
nucleoplasmTP53-binding protein 1Homo sapiens (human)
replication forkTP53-binding protein 1Homo sapiens (human)
cytoplasmTP53-binding protein 1Homo sapiens (human)
nuclear bodyTP53-binding protein 1Homo sapiens (human)
site of double-strand breakTP53-binding protein 1Homo sapiens (human)
DNA repair complexTP53-binding protein 1Homo sapiens (human)
nucleusTP53-binding protein 1Homo sapiens (human)
nucleusLethal(3)malignant brain tumor-like protein 4Homo sapiens (human)
nucleusLethal(3)malignant brain tumor-like protein 3Homo sapiens (human)
nucleoplasmLethal(3)malignant brain tumor-like protein 3Homo sapiens (human)
nucleolusLethal(3)malignant brain tumor-like protein 3Homo sapiens (human)
spindleE3 ubiquitin-protein ligase UHRF1Homo sapiens (human)
nucleusE3 ubiquitin-protein ligase UHRF1Homo sapiens (human)
nucleoplasmE3 ubiquitin-protein ligase UHRF1Homo sapiens (human)
replication forkE3 ubiquitin-protein ligase UHRF1Homo sapiens (human)
nuclear matrixE3 ubiquitin-protein ligase UHRF1Homo sapiens (human)
chromatinE3 ubiquitin-protein ligase UHRF1Homo sapiens (human)
euchromatinE3 ubiquitin-protein ligase UHRF1Homo sapiens (human)
heterochromatinE3 ubiquitin-protein ligase UHRF1Homo sapiens (human)
nucleoplasmPHD finger protein 23Homo sapiens (human)
cytoplasmPHD finger protein 23Homo sapiens (human)
nucleusPHD finger protein 23Homo sapiens (human)
nucleusScm-like with four MBT domains protein 1Homo sapiens (human)
nucleoplasmScm-like with four MBT domains protein 1Homo sapiens (human)
nucleusScm-like with four MBT domains protein 1Homo sapiens (human)
nucleolusLethal(3)malignant brain tumor-like protein 1Homo sapiens (human)
condensed chromosomeLethal(3)malignant brain tumor-like protein 1Homo sapiens (human)
nucleusLethal(3)malignant brain tumor-like protein 1Homo sapiens (human)
nucleoplasmLethal(3)malignant brain tumor-like protein 1Homo sapiens (human)
chromatin lock complexLethal(3)malignant brain tumor-like protein 1Homo sapiens (human)
chromatinLethal(3)malignant brain tumor-like protein 1Homo sapiens (human)
nucleusLethal(3)malignant brain tumor-like protein 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (68)

Assay IDTitleYearJournalArticle
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: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
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
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
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
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845Primary qHTS for Inhibitors of ATXN expression
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
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
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
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
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
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
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
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
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
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
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
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
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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
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
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
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
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
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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
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
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
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
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
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
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID771614Inhibition of UHRF1 (unknown origin) after 30 mins by AlphaScreen assay2013Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
Small-molecule ligands of methyl-lysine binding proteins: optimization of selectivity for L3MBTL3.
AID1077874Inhibition of 53BP1 (1485 to 1611) (unknown origin) expressed in Escherichia coli BL21 Rosetta DE3 using H4K20Me2 as substrate incubated for 30 mins at room temperature followed by incubation under dark condition for 30 mins by AlphaScreen assay2013MedChemComm, Nov, Volume: 4, Issue:11
The structure-activity relationships of L3MBTL3 inhibitors: flexibility of the dimer interface.
AID593469Binding affinity to L3MBTL3 by chemiluminescent assay2011Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
Small-molecule ligands of methyl-lysine binding proteins.
AID1077871Inhibition of GST-tagged Jarid1A (unknown origin) using H3K4Me3 as substrate incubated for 30 mins at room temperature followed by incubation under dark condition for 30 mins by AlphaScreen assay2013MedChemComm, Nov, Volume: 4, Issue:11
The structure-activity relationships of L3MBTL3 inhibitors: flexibility of the dimer interface.
AID1077873Inhibition of CBX7 (8 to 62) (unknown origin) expressed in Escherichia coli BL21 Rosetta DE3 using H3K9Me3 as substrate incubated for 30 mins at room temperature followed by incubation under dark condition for 30 mins by AlphaScreen assay2013MedChemComm, Nov, Volume: 4, Issue:11
The structure-activity relationships of L3MBTL3 inhibitors: flexibility of the dimer interface.
AID771617Inhibition of SFMBT1 (unknown origin) after 30 mins by AlphaScreen assay2013Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
Small-molecule ligands of methyl-lysine binding proteins: optimization of selectivity for L3MBTL3.
AID1654638Substrate activity at aldehyde oxidase in human liver cytosol assessed as mono-oxide metabolite formation at 10 uM measured after 3 hrs in presence of XO inhibitor allopurinol by UPLC/Q-TOF MS analysis2020Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12
Revisiting Aldehyde Oxidase Mediated Metabolism in Drug-like Molecules: An Improved Computational Model.
AID593467Selectivity for human L3MBTL1 over human L3MBTL42011Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
Small-molecule ligands of methyl-lysine binding proteins.
AID593466Selectivity for human L3MBTL1 over human L3MBTL32011Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
Small-molecule ligands of methyl-lysine binding proteins.
AID593468Binding affinity to human L3MBTL1 by chemiluminescent assay2011Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
Small-molecule ligands of methyl-lysine binding proteins.
AID1077870Inhibition of GST-tagged PHF23 (unknown origin) using H3K4Me3 as substrate incubated for 30 mins at room temperature followed by incubation under dark condition for 30 mins by AlphaScreen assay2013MedChemComm, Nov, Volume: 4, Issue:11
The structure-activity relationships of L3MBTL3 inhibitors: flexibility of the dimer interface.
AID593544Binding affinity to CBX7 by chemiluminescent assay2011Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
Small-molecule ligands of methyl-lysine binding proteins.
AID771619Inhibition of L3MBTL1 (unknown origin) after 30 mins by AlphaScreen assay2013Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
Small-molecule ligands of methyl-lysine binding proteins: optimization of selectivity for L3MBTL3.
AID1654634Substrate activity at aldehyde oxidase in human liver cytosol assessed as mono-oxide metabolite formation at 10 uM measured after 3 hrs by LC-MS analysis2020Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12
Revisiting Aldehyde Oxidase Mediated Metabolism in Drug-like Molecules: An Improved Computational Model.
AID1654632Substrate activity at aldehyde oxidase in human liver cytosol at 10 uM measured after 3 hrs by UPLC/Q-TOF MS analysis2020Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12
Revisiting Aldehyde Oxidase Mediated Metabolism in Drug-like Molecules: An Improved Computational Model.
AID593542Binding affinity to MBTD1 by chemiluminescent assay2011Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
Small-molecule ligands of methyl-lysine binding proteins.
AID1654636Substrate activity at aldehyde oxidase in human liver cytosol assessed as mono-oxide metabolite formation at 10 uM measured after 3 hrs in presence of AOX inhibitor raloxifene by UPLC/Q-TOF MS analysis2020Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12
Revisiting Aldehyde Oxidase Mediated Metabolism in Drug-like Molecules: An Improved Computational Model.
AID593545Displacement of FAM-AHA-ARTKQTARK(Me)STGGKA-CO2H from human L3MBTL1 assessed as apparent dissociation constant after 20 mins by FP-displacement Assay2011Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
Small-molecule ligands of methyl-lysine binding proteins.
AID1077875Inhibition of MBTD1 (130 to 566) (unknown origin) expressed in Escherichia coli BL21 Rosetta DE3 using H4K20Me1 as substrate incubated for 30 mins at room temperature followed by incubation under dark condition for 30 mins by AlphaScreen assay2013MedChemComm, Nov, Volume: 4, Issue:11
The structure-activity relationships of L3MBTL3 inhibitors: flexibility of the dimer interface.
AID771611Inhibition of JARID1A (unknown origin) after 30 mins by AlphaScreen assay2013Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
Small-molecule ligands of methyl-lysine binding proteins: optimization of selectivity for L3MBTL3.
AID593463Binding affinity to human L3MBTL1 assessed as dissociation constant by isothermal titration calorimetric assay2011Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
Small-molecule ligands of methyl-lysine binding proteins.
AID771616Inhibition of CBX7 (unknown origin) after 30 mins by AlphaScreen assay2013Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
Small-molecule ligands of methyl-lysine binding proteins: optimization of selectivity for L3MBTL3.
AID771612Inhibition of PHF23 (unknown origin) after 30 mins by AlphaScreen assay2013Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
Small-molecule ligands of methyl-lysine binding proteins: optimization of selectivity for L3MBTL3.
AID1077876Inhibition of His-tagged L3MBTL1 (unknown origin) using H4K20Me1 as substrate incubated for 30 mins at room temperature followed by incubation under dark condition for 30 mins by AlphaScreen assay2013MedChemComm, Nov, Volume: 4, Issue:11
The structure-activity relationships of L3MBTL3 inhibitors: flexibility of the dimer interface.
AID1077872Inhibition of UHRF1 tandem tudor domain (121 to 286) (unknown origin) expressed in Escherichia coli BL21 Rosetta DE3 using H3K9Me3 as substrate incubated for 30 mins at room temperature followed by incubation under dark condition for 30 mins by AlphaScree2013MedChemComm, Nov, Volume: 4, Issue:11
The structure-activity relationships of L3MBTL3 inhibitors: flexibility of the dimer interface.
AID771620Inhibition of L3MBTL3 (unknown origin) after 30 mins by AlphaScreen assay2013Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
Small-molecule ligands of methyl-lysine binding proteins: optimization of selectivity for L3MBTL3.
AID1654637Substrate activity at aldehyde oxidase in human liver cytosol assessed as mono-oxide metabolite formation at 10 uM measured after 3 hrs in presence of AOX inhibitor hydralazine by UPLC/Q-TOF MS analysis2020Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12
Revisiting Aldehyde Oxidase Mediated Metabolism in Drug-like Molecules: An Improved Computational Model.
AID771618Inhibition of L3MBTL4 (unknown origin) after 30 mins by AlphaScreen assay2013Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
Small-molecule ligands of methyl-lysine binding proteins: optimization of selectivity for L3MBTL3.
AID593541Binding affinity to human SFMBT by chemiluminescent assay2011Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
Small-molecule ligands of methyl-lysine binding proteins.
AID771615Inhibition of MBTD1 (unknown origin) after 30 mins by AlphaScreen assay2013Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
Small-molecule ligands of methyl-lysine binding proteins: optimization of selectivity for L3MBTL3.
AID593543Binding affinity to PHF13 by chemiluminescent assay2011Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
Small-molecule ligands of methyl-lysine binding proteins.
AID771621Inhibition of L3MBTL3 (unknown origin) using H4K20me2 as substrate after 30 mins by LNCE-TR-FRET assay2013Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
Small-molecule ligands of methyl-lysine binding proteins: optimization of selectivity for L3MBTL3.
AID1654635Substrate activity at aldehyde oxidase in human liver cytosol assessed as mono-oxide metabolite formation at 10 uM measured after 3 hrs by UPLC/Q-TOF MS analysis2020Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12
Revisiting Aldehyde Oxidase Mediated Metabolism in Drug-like Molecules: An Improved Computational Model.
AID593540Binding affinity to L3MBTL4 by chemiluminescent assay2011Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
Small-molecule ligands of methyl-lysine binding proteins.
AID1077877Inhibition of His-tagged L3MBTL3 (unknown origin) using H4K20Me2 as substrate incubated for 30 mins at room temperature followed by incubation under dark condition for 30 mins by AlphaScreen assay2013MedChemComm, Nov, Volume: 4, Issue:11
The structure-activity relationships of L3MBTL3 inhibitors: flexibility of the dimer interface.
AID771613Inhibition of 53BP1 (unknown origin) after 30 mins by AlphaScreen assay2013Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
Small-molecule ligands of methyl-lysine binding proteins: optimization of selectivity for L3MBTL3.
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.
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.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (12)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's5 (41.67)24.3611
2020's7 (58.33)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 11.98

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 Index11.98 (24.57)
Research Supply Index2.56 (2.92)
Research Growth Index4.54 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.98)

All Compounds (24.57)

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%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]