Page last updated: 2024-12-11

gr 159897

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

Description

GR 159897: a selective non-peptide antagonist at tachykinin NK2 receptors; structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID9953599
CHEMBL ID2110370
CHEBI ID92912
MeSH IDM0245357

Synonyms (24)

Synonym
gr-159,897
5-fluoro-3-[2-[4-methoxy-4-[[(r)-phenylsulfinyl]methyl]piperidin-1-yl]ethyl]-1h-indole
gtpl2115
gr-159897
gr 159897
CHEMBL2110370 ,
AKOS025147300
3-[2-(4-(r)-benzenesulfinylmethyl-4-methoxy-piperidin-1-yl)-ethyl]-5-fluoro-1h-indole
AKOS024456505
SR-01000597395-1
sr-01000597395
CHEBI:92912
NCGC00381706-02
(r)-1-[2-(5-fluoro-1h-indol-3-yl) ethyl]-4-methoxy -4-[(phenyl-sulfinyl)methyl]-piperidine
5-fluoro-3-[2-[4-methoxy-4-[[(r)phenylsulfinyl]methyl]-1-piperidinyl]ethyl]-1h-indole
5-fluoro-3-[2-[4-methoxy-4-[[?-phenylsulphinyl]methyl]-1-piperidinyl]ethyl]-1h-indole
(r)-5-fluoro-3-(2-(4-methoxy-4-(phenylsulfinylmethyl)piperidin-1-yl)ethyl)-1h-indole
(r)-5-fluoro-3-(2-(4-methoxy-4-((phenylsulfinyl)methyl)piperidin-1-yl)ethyl)-1h-indole
bdbm50212987
Q27077844
HY-107691
HMS3412E06
CS-0029221
E98748

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 (1)

ClassDescription
tryptaminesTryptamine and its substitution derivatives.
[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 (1)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
cytochrome P450 2D6Homo sapiens (human)Potency2.39190.00108.379861.1304AID1645840
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (8)

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.
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.
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.
AID1346371Human NK2 receptor (Tachykinin receptors)1995European journal of pharmacology, Jan-16, Volume: 272, Issue:2-3
GR159897, a potent non-peptide antagonist at tachykinin NK2 receptors.
AID1346371Human NK2 receptor (Tachykinin receptors)1993Biochemical and biophysical research communications, Mar-31, Volume: 191, Issue:3
Characterization of the binding sites of [3H]SR 48968, a potent nonpeptide radioligand antagonist of the neurokinin-2 receptor.
AID1346371Human NK2 receptor (Tachykinin receptors)1995Journal of medicinal chemistry, Sep-15, Volume: 38, Issue:19
New spiropiperidines as potent and selective non-peptide tachykinin NK2 receptor antagonists.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (18)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's6 (33.33)18.2507
2000's2 (11.11)29.6817
2010's8 (44.44)24.3611
2020's2 (11.11)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

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%
Other18 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]