Page last updated: 2024-11-12

rs 504393

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

Description

RS 504393: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID9953769
CHEMBL ID134074
CHEBI ID93525
SCHEMBL ID9972645
MeSH IDM0582381

Synonyms (35)

Synonym
HY-15418
HMS3269M19
BRD-K87510569-001-01-0
6-methyl-1'-[2-(5-methyl-2-phenyl-1,3-oxazol-4-yl)ethyl]-1,2-dihydrospiro[3,1-benzoxazine-4,4'-piperidine]-2-one
gtpl781
rs504393
rs-504393
AKOS015842093
NCGC00167758-01
bdbm50133111
6-methyl-1''-[2-(5-methyl-2-phenyl-1,3-oxazol-4-yl)ethyl]spiro[1,4-dihydro-2h-benzo[d][1,3]oxazine-4,4''-(hexahydropyridine)]-2-one
CHEMBL134074 ,
300816-15-3
rs 504393
BCPP000086
CS-0851
6-methyl-1'-(2-(5-methyl-2-phenyloxazol-4-yl)ethyl)spiro[benzo[d][1,3]oxazine-4,4'-piperidin]-2(1h)-one
6-methyl-1'-[2-(5-methyl-2-phenyl-4-oxazolyl)ethyl]spiro[4h-3,1-benzoxazine-4,4'-piperidin]-2(1h)-one
SCHEMBL9972645
6-methyl-1'-[2-(5-methyl-2-phenyl-4-oxazolyl)ethyl]-spiro[4h-3,1-benzoxazine-4,4'-piperidin]-2(1h)-one
DTXSID20433290
6-methyl-1'-[2-(5-methyl-2-phenyl-1,3-oxazol-4-yl)ethyl]spiro[3,1-benzoxazine-4,4'-piperidin]-2(1h)-one
CHEBI:93525
6-methyl-1'-[2-(5-methyl-2-phenyl-1,3-oxazol-4-yl)ethyl]-1,2-dihydrospiro[3,1-benzoxazine-4,4'-piperidin]-2-one
AS-74752
spiro[4h-3,1-benzoxazine-4,4'-piperidin]-2(1h)-one,6-methyl-1'-[2-(5-methyl-2-phenyl-4-oxazolyl)ethyl]-
6-methyl-1'-(2-(5-methyl-2-phenyloxazol-4-yl)ethyl)spiro-[benzo[d][1,3]oxazine-4,4'-piperidin]-2(1h)-one
HMS3677F05
mfcd09038564
Q27088636
BCP02713
HMS3413F05
NCGC00167758-06
6-methyl-1'-[2-(5-methyl-2-phenyl-1,3-oxazol-4-yl)ethyl]spiro[1h-3,1-benzoxazine-4,4'-piperidine]-2-one
EX-A8014F
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
1,3-oxazoles
[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 (3)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, TYROSYL-DNA PHOSPHODIESTERASEHomo sapiens (human)Potency89.12510.004023.8416100.0000AID485290
[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)
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)Ki0.29180.00010.739610.0000AID43218; AID43226
C-C chemokine receptor type 2Homo sapiens (human)IC50 (µMol)0.08900.00000.67366.6990AID44755
C-C chemokine receptor type 2Homo sapiens (human)Ki1.25610.00200.84276.3096AID43210; AID43214; AID43216; AID43217; AID43218; AID43220; AID43226; AID44761; AID44762
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (54)

Processvia Protein(s)Taxonomy
cytokine-mediated signaling pathwayC-C chemokine receptor type 2Homo sapiens (human)
blood vessel remodelingC-C chemokine receptor type 2Homo sapiens (human)
dendritic cell chemotaxisC-C chemokine receptor type 2Homo sapiens (human)
monocyte chemotaxisC-C chemokine receptor type 2Homo sapiens (human)
regulation of T cell cytokine productionC-C chemokine receptor type 2Homo sapiens (human)
positive regulation of T-helper 1 type immune responseC-C chemokine receptor type 2Homo sapiens (human)
negative regulation of type 2 immune responseC-C chemokine receptor type 2Homo sapiens (human)
intracellular calcium ion homeostasisC-C chemokine receptor type 2Homo sapiens (human)
chemotaxisC-C chemokine receptor type 2Homo sapiens (human)
humoral immune responseC-C chemokine receptor type 2Homo sapiens (human)
cellular defense responseC-C chemokine receptor type 2Homo sapiens (human)
negative regulation of adenylate cyclase activityC-C chemokine receptor type 2Homo sapiens (human)
cell surface receptor signaling pathway via JAK-STATC-C chemokine receptor type 2Homo sapiens (human)
response to woundingC-C chemokine receptor type 2Homo sapiens (human)
regulation of vascular endothelial growth factor productionC-C chemokine receptor type 2Homo sapiens (human)
positive regulation of T cell chemotaxisC-C chemokine receptor type 2Homo sapiens (human)
negative regulation of angiogenesisC-C chemokine receptor type 2Homo sapiens (human)
sensory perception of painC-C chemokine receptor type 2Homo sapiens (human)
cellular homeostasisC-C chemokine receptor type 2Homo sapiens (human)
hemopoiesisC-C chemokine receptor type 2Homo sapiens (human)
positive regulation of type II interferon productionC-C chemokine receptor type 2Homo sapiens (human)
positive regulation of interleukin-2 productionC-C chemokine receptor type 2Homo sapiens (human)
positive regulation of tumor necrosis factor productionC-C chemokine receptor type 2Homo sapiens (human)
monocyte extravasationC-C chemokine receptor type 2Homo sapiens (human)
T-helper 17 cell chemotaxisC-C chemokine receptor type 2Homo sapiens (human)
negative regulation of eosinophil degranulationC-C chemokine receptor type 2Homo sapiens (human)
regulation of T cell differentiationC-C chemokine receptor type 2Homo sapiens (human)
positive regulation of alpha-beta T cell proliferationC-C chemokine receptor type 2Homo sapiens (human)
homeostasis of number of cells within a tissueC-C chemokine receptor type 2Homo sapiens (human)
regulation of inflammatory responseC-C chemokine receptor type 2Homo sapiens (human)
positive regulation of inflammatory responseC-C chemokine receptor type 2Homo sapiens (human)
positive regulation of T cell activationC-C chemokine receptor type 2Homo sapiens (human)
positive regulation of synaptic transmission, glutamatergicC-C chemokine receptor type 2Homo sapiens (human)
leukocyte adhesion to vascular endothelial cellC-C chemokine receptor type 2Homo sapiens (human)
chemokine-mediated signaling pathwayC-C chemokine receptor type 2Homo sapiens (human)
positive regulation of monocyte chemotaxisC-C chemokine receptor type 2Homo sapiens (human)
positive regulation of immune complex clearance by monocytes and macrophagesC-C chemokine receptor type 2Homo sapiens (human)
inflammatory response to woundingC-C chemokine receptor type 2Homo sapiens (human)
neutrophil clearanceC-C chemokine receptor type 2Homo sapiens (human)
positive regulation of cold-induced thermogenesisC-C chemokine receptor type 2Homo sapiens (human)
positive regulation of leukocyte tethering or rollingC-C chemokine receptor type 2Homo sapiens (human)
positive regulation of NMDA glutamate receptor activityC-C chemokine receptor type 2Homo sapiens (human)
macrophage migrationC-C chemokine receptor type 2Homo sapiens (human)
regulation of macrophage migrationC-C chemokine receptor type 2Homo sapiens (human)
positive regulation of thymocyte migrationC-C chemokine receptor type 2Homo sapiens (human)
positive regulation of monocyte extravasationC-C chemokine receptor type 2Homo sapiens (human)
positive regulation of CD8-positive, alpha-beta T cell extravasationC-C chemokine receptor type 2Homo sapiens (human)
positive regulation of astrocyte chemotaxisC-C chemokine receptor type 2Homo sapiens (human)
positive regulation of hematopoietic stem cell migrationC-C chemokine receptor type 2Homo sapiens (human)
cell chemotaxisC-C chemokine receptor type 2Homo sapiens (human)
calcium-mediated signalingC-C chemokine receptor type 2Homo sapiens (human)
inflammatory responseC-C chemokine receptor type 2Homo sapiens (human)
immune responseC-C chemokine receptor type 2Homo sapiens (human)
positive regulation of cytosolic calcium ion concentrationC-C chemokine receptor type 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (9)

Processvia Protein(s)Taxonomy
chemokine receptor activityC-C chemokine receptor type 2Homo sapiens (human)
protein bindingC-C chemokine receptor type 2Homo sapiens (human)
CCR2 chemokine receptor bindingC-C chemokine receptor type 2Homo sapiens (human)
chemokine (C-C motif) ligand 2 bindingC-C chemokine receptor type 2Homo sapiens (human)
chemokine (C-C motif) ligand 12 bindingC-C chemokine receptor type 2Homo sapiens (human)
chemokine (C-C motif) ligand 7 bindingC-C chemokine receptor type 2Homo sapiens (human)
identical protein bindingC-C chemokine receptor type 2Homo sapiens (human)
C-C chemokine bindingC-C chemokine receptor type 2Homo sapiens (human)
C-C chemokine receptor activityC-C chemokine receptor type 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (10)

Processvia Protein(s)Taxonomy
fibrillar centerC-C chemokine receptor type 2Homo sapiens (human)
cytoplasmC-C chemokine receptor type 2Homo sapiens (human)
cytosolC-C chemokine receptor type 2Homo sapiens (human)
plasma membraneC-C chemokine receptor type 2Homo sapiens (human)
membraneC-C chemokine receptor type 2Homo sapiens (human)
dendriteC-C chemokine receptor type 2Homo sapiens (human)
neuronal cell bodyC-C chemokine receptor type 2Homo sapiens (human)
perikaryonC-C chemokine receptor type 2Homo sapiens (human)
perinuclear region of cytoplasmC-C chemokine receptor type 2Homo sapiens (human)
cytoplasmC-C chemokine receptor type 2Homo sapiens (human)
external side of plasma membraneC-C chemokine receptor type 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (21)

Assay IDTitleYearJournalArticle
AID1508628Confirmatory 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.
AID1508629Cell Viability qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
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.
AID1508627Counterscreen qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: GLuc-NoTag assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
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.
AID43216Binding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells2003Journal of medicinal chemistry, Sep-11, Volume: 46, Issue:19
CCR2: characterization of the antagonist binding site from a combined receptor modeling/mutagenesis approach.
AID43218Binding affinity of compound (10 uM) towards T290A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells2003Journal of medicinal chemistry, Sep-11, Volume: 46, Issue:19
CCR2: characterization of the antagonist binding site from a combined receptor modeling/mutagenesis approach.
AID43214Binding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells2003Journal of medicinal chemistry, Sep-11, Volume: 46, Issue:19
CCR2: characterization of the antagonist binding site from a combined receptor modeling/mutagenesis approach.
AID43217Binding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells2003Journal of medicinal chemistry, Sep-11, Volume: 46, Issue:19
CCR2: characterization of the antagonist binding site from a combined receptor modeling/mutagenesis approach.
AID43220Binding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells2003Journal of medicinal chemistry, Sep-11, Volume: 46, Issue:19
CCR2: characterization of the antagonist binding site from a combined receptor modeling/mutagenesis approach.
AID43224Binding affinity of compound (10 uM) towards Y210A-292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells: Inactive2003Journal of medicinal chemistry, Sep-11, Volume: 46, Issue:19
CCR2: characterization of the antagonist binding site from a combined receptor modeling/mutagenesis approach.
AID44762Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2)2003Journal of medicinal chemistry, Sep-11, Volume: 46, Issue:19
CCR2: characterization of the antagonist binding site from a combined receptor modeling/mutagenesis approach.
AID43222Binding affinity of compound (10 uM) towards Y1210A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells; Inactive2003Journal of medicinal chemistry, Sep-11, Volume: 46, Issue:19
CCR2: characterization of the antagonist binding site from a combined receptor modeling/mutagenesis approach.
AID44755Inhibitory activity against C-C chemokine receptor type 2 (antagonist activity)2003Journal of medicinal chemistry, Sep-11, Volume: 46, Issue:19
CCR2: characterization of the antagonist binding site from a combined receptor modeling/mutagenesis approach.
AID44760Inhibition of chemotaxis by C-C chemokine receptor type 2 antagonist in human monocytes was measured in the presence 1 nM MCP-12003Journal of medicinal chemistry, Sep-11, Volume: 46, Issue:19
CCR2: characterization of the antagonist binding site from a combined receptor modeling/mutagenesis approach.
AID43210Binding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells2003Journal of medicinal chemistry, Sep-11, Volume: 46, Issue:19
CCR2: characterization of the antagonist binding site from a combined receptor modeling/mutagenesis approach.
AID43226Binding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells2003Journal of medicinal chemistry, Sep-11, Volume: 46, Issue:19
CCR2: characterization of the antagonist binding site from a combined receptor modeling/mutagenesis approach.
AID44761Binding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cells2003Journal of medicinal chemistry, Sep-11, Volume: 46, Issue:19
CCR2: characterization of the antagonist binding site from a combined receptor modeling/mutagenesis approach.
AID43212Binding affinity of compound (10 uM) towards E291Q receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells: Inactive2003Journal of medicinal chemistry, Sep-11, Volume: 46, Issue:19
CCR2: characterization of the antagonist binding site from a combined receptor modeling/mutagenesis approach.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).2014Journal of biomolecular screening, Jul, Volume: 19, Issue:6
A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (31)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's1 (3.23)29.6817
2010's20 (64.52)24.3611
2020's10 (32.26)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 28.78

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 Index28.78 (24.57)
Research Supply Index3.50 (2.92)
Research Growth Index6.48 (4.65)
Search Engine Demand Index25.99 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (28.78)

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%
Other32 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]