Page last updated: 2024-11-12

bms 193885

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

Description

BMS 193885: a neuropeptide YY1 receptor antagonist; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID9960164
MeSH IDM0426858
PubMed CID56972234
MeSH IDM0426858

Synonyms (33)

Synonym
bms-193885
HMS3263K13
186185-03-5
CCG-222320
819srg2y6n ,
3,5-pyridinedicarboxylic acid, 1,4-dihydro-4-(3-((((3-(4-(3-methoxyphenyl)-1-piperidinyl)propyl)amino)carbonyl)amino)phenyl)-2,6-dimethyl-, dimethyl ester
unii-819srg2y6n
3,5-pyridinedicarboxylic acid, 1,4-dihydro-4-(3-((((3-(4-(3-methoxyphenyl)-1-piperidinyl)propyl)amino)carbonyl)amino)phenyl)-2,6-dimethyl-, 3,5-dimethyl ester
tox21_501016
NCGC00261701-01
bms-193885, >=98% (hplc)
NCGC00485144-01
EX-A7102
HY-120619
DTXSID501018102
NCGC00485144-02
CS-0078457
Q27269229
MS-30521
dimethyl 4-[3-[3-[4-(3-methoxyphenyl)piperidin-1-yl]propylcarbamoylamino]phenyl]-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate
1,4-dihydro-4-[3-[[[[3-[4-(3-methoxyphenyl)-1-piperidinyl]propyl]amino]carbonyl]amino]phenyl]-2,6-dimethyl-3,5-pyridinedicarboxylicacid3,5-dimethylesterl-lactate
AKOS040741386
1,4-dihydro-4-[3-[[[[3-[4-(3-methoxyphenyl)-1-piperidinyl]propyl]amino]carbonyl]amino]phenyl]-2,6-dimethyl-3,5-pyridinedicarboxylic acid 3,5-dimethyl ester l-lactate
bms 193885
AKOS024457502
679839-66-8
J-011947
bms193885
dimethyl 4-[3-[3-[4-(3-methoxyphenyl)piperidin-1-yl]propylcarbamoylamino]phenyl]-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate;(2s)-2-hydroxypropanoic acid
EX-A6700
CS-0029395
bms-193885 (l-lactic acid)
HY-107727

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]

Protein Targets (7)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Fumarate hydrataseHomo sapiens (human)Potency35.48130.00308.794948.0869AID1347053
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency24.51210.001530.607315,848.9004AID1224819; AID1224820; AID1224821; AID1224823
polyproteinZika virusPotency35.48130.00308.794948.0869AID1347053
[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)
Neuropeptide Y receptor type 1Homo sapiens (human)IC50 (µMol)0.00420.00020.70318.3700AID146439
Neuropeptide Y receptor type 1Homo sapiens (human)Ki0.00330.00010.22952.3150AID146581
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Neuropeptide Y receptor type 1Homo sapiens (human)Kb0.00450.00150.00210.0045AID146576
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (23)

Processvia Protein(s)Taxonomy
outflow tract morphogenesisNeuropeptide Y receptor type 1Homo sapiens (human)
glucose metabolic processNeuropeptide Y receptor type 1Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerNeuropeptide Y receptor type 1Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayNeuropeptide Y receptor type 1Homo sapiens (human)
neuropeptide signaling pathwayNeuropeptide Y receptor type 1Homo sapiens (human)
locomotory behaviorNeuropeptide Y receptor type 1Homo sapiens (human)
feeding behaviorNeuropeptide Y receptor type 1Homo sapiens (human)
regulation of blood pressureNeuropeptide Y receptor type 1Homo sapiens (human)
sensory perception of painNeuropeptide Y receptor type 1Homo sapiens (human)
regulation of multicellular organism growthNeuropeptide Y receptor type 1Homo sapiens (human)
outflow tract morphogenesisNeuropeptide Y receptor type 2Homo sapiens (human)
cardiac left ventricle morphogenesisNeuropeptide Y receptor type 2Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayNeuropeptide Y receptor type 2Homo sapiens (human)
neuropeptide signaling pathwayNeuropeptide Y receptor type 2Homo sapiens (human)
locomotory behaviorNeuropeptide Y receptor type 2Homo sapiens (human)
G protein-coupled receptor signaling pathwayNeuropeptide Y receptor type 4Homo sapiens (human)
neuropeptide signaling pathwayNeuropeptide Y receptor type 4Homo sapiens (human)
positive regulation of acute inflammatory responseNeuropeptide Y receptor type 5Homo sapiens (human)
negative regulation of acute inflammatory response to antigenic stimulusNeuropeptide Y receptor type 5Homo sapiens (human)
outflow tract morphogenesisNeuropeptide Y receptor type 5Homo sapiens (human)
cardiac left ventricle morphogenesisNeuropeptide Y receptor type 5Homo sapiens (human)
neuropeptide signaling pathwayNeuropeptide Y receptor type 5Homo sapiens (human)
negative regulation of glutamate secretionNeuropeptide Y receptor type 5Homo sapiens (human)
negative regulation of synaptic transmission, GABAergicNeuropeptide Y receptor type 5Homo sapiens (human)
eating behaviorNeuropeptide Y receptor type 5Homo sapiens (human)
negative regulation of apoptotic processNeuropeptide Y receptor type 5Homo sapiens (human)
positive regulation of smooth muscle cell proliferationNeuropeptide Y receptor type 5Homo sapiens (human)
generation of ovulation cycle rhythmNeuropeptide Y receptor type 5Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeNeuropeptide Y receptor type 5Homo sapiens (human)
synaptic signaling via neuropeptideNeuropeptide Y receptor type 5Homo sapiens (human)
chemical synaptic transmissionNeuropeptide Y receptor type 5Homo sapiens (human)
G protein-coupled receptor signaling pathwayNeuropeptide Y receptor type 5Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (10)

Processvia Protein(s)Taxonomy
peptide YY receptor activityNeuropeptide Y receptor type 1Homo sapiens (human)
pancreatic polypeptide receptor activityNeuropeptide Y receptor type 1Homo sapiens (human)
neuropeptide Y receptor activityNeuropeptide Y receptor type 1Homo sapiens (human)
protein bindingNeuropeptide Y receptor type 1Homo sapiens (human)
neuropeptide receptor activityNeuropeptide Y receptor type 1Homo sapiens (human)
neuropeptide bindingNeuropeptide Y receptor type 1Homo sapiens (human)
peptide YY receptor activityNeuropeptide Y receptor type 2Homo sapiens (human)
neuropeptide Y receptor activityNeuropeptide Y receptor type 2Homo sapiens (human)
calcium channel regulator activityNeuropeptide Y receptor type 2Homo sapiens (human)
protein bindingNeuropeptide Y receptor type 2Homo sapiens (human)
signaling receptor activityNeuropeptide Y receptor type 2Homo sapiens (human)
pancreatic polypeptide receptor activityNeuropeptide Y receptor type 4Homo sapiens (human)
G protein-coupled receptor activityNeuropeptide Y receptor type 4Homo sapiens (human)
peptide hormone bindingNeuropeptide Y receptor type 4Homo sapiens (human)
neuropeptide bindingNeuropeptide Y receptor type 4Homo sapiens (human)
neuropeptide Y receptor activityNeuropeptide Y receptor type 5Homo sapiens (human)
pancreatic polypeptide receptor activityNeuropeptide Y receptor type 5Homo sapiens (human)
peptide YY receptor activityNeuropeptide Y receptor type 5Homo sapiens (human)
neuropeptide bindingNeuropeptide Y receptor type 5Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (7)

Processvia Protein(s)Taxonomy
plasma membraneNeuropeptide Y receptor type 1Homo sapiens (human)
plasma membraneNeuropeptide Y receptor type 1Homo sapiens (human)
neuron projectionNeuropeptide Y receptor type 1Homo sapiens (human)
plasma membraneNeuropeptide Y receptor type 2Homo sapiens (human)
ciliumNeuropeptide Y receptor type 2Homo sapiens (human)
non-motile ciliumNeuropeptide Y receptor type 2Homo sapiens (human)
plasma membraneNeuropeptide Y receptor type 4Homo sapiens (human)
membraneNeuropeptide Y receptor type 4Homo sapiens (human)
neuron projectionNeuropeptide Y receptor type 4Homo sapiens (human)
plasma membraneNeuropeptide Y receptor type 4Homo sapiens (human)
plasma membraneNeuropeptide Y receptor type 5Homo sapiens (human)
presynapseNeuropeptide Y receptor type 5Homo sapiens (human)
GABA-ergic synapseNeuropeptide Y receptor type 5Homo sapiens (human)
plasma membraneNeuropeptide Y receptor type 5Homo sapiens (human)
neuron projectionNeuropeptide Y receptor type 5Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (31)

Assay IDTitleYearJournalArticle
AID1347153Confirmatory 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.
AID1347057CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347169Tertiary RLuc qRT-PCR qHTS assay 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.
AID1347059CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347152Confirmatory screen NINDS 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.
AID1347168HepG2 cells viability 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.
AID1347405qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection2020ACS 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.
AID1347161Confirmatory 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.
AID1347167Vero cells viability 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.
AID1347410qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library2019Cellular signalling, 08, Volume: 60A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening.
AID1347058CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347151Optimization of GU AMC 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.
AID1347149Furin counterscreen 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.
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.
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.
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.
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.
AID146736Binding affinity for human Neuropeptide Y4 receptor; No affinity2002Bioorganic & medicinal chemistry letters, Feb-11, Volume: 12, Issue:3
Dihydropyridine neuropeptide Y Y(1) receptor antagonists.
AID174813Ability to decrease spontaneous nocturnal food intake at 10 mg/kg (ip) in rats2002Bioorganic & medicinal chemistry letters, Feb-11, Volume: 12, Issue:3
Dihydropyridine neuropeptide Y Y(1) receptor antagonists.
AID146767Binding affinity for human Neuropeptide Y5 receptor; No affinity2002Bioorganic & medicinal chemistry letters, Feb-11, Volume: 12, Issue:3
Dihydropyridine neuropeptide Y Y(1) receptor antagonists.
AID669655Competitive displacement of [125I]peptideYY from NPY1 receptor in human SK-N-MC cells at 50 nM by equilibrium binding assay2012ACS medicinal chemistry letters, Mar-08, Volume: 3, Issue:3
Discovery of a Novel Class of Bicyclo[3.1.0]hexanylpiperazines as Noncompetitive Neuropeptide Y Y1 Antagonists.
AID146581Inhibition of binding of [125I]PYY radioligand to human neuropeptide Y1 receptor in SK-N-MC cell membrane2002Bioorganic & medicinal chemistry letters, Feb-11, Volume: 12, Issue:3
Dihydropyridine neuropeptide Y Y(1) receptor antagonists.
AID174814Ability to decrease spontaneous nocturnal food intake at 20 mg/kg (ip) in rats2002Bioorganic & medicinal chemistry letters, Feb-11, Volume: 12, Issue:3
Dihydropyridine neuropeptide Y Y(1) receptor antagonists.
AID174816Ability to inhibit food consumption increased by 10 ug icv infusion of NPY followed by compound administered at 30 mg/kg (ip) in satiated rats2002Bioorganic & medicinal chemistry letters, Feb-11, Volume: 12, Issue:3
Dihydropyridine neuropeptide Y Y(1) receptor antagonists.
AID146439Binding affinity against Neuropeptide Y receptor type 1 using I-PYY as a radioligand in human neuroblastoma SK-N-MC cells2002Bioorganic & medicinal chemistry letters, Feb-11, Volume: 12, Issue:3
Novel dihydropyrazine analogues as NPY antagonists.
AID174815Ability to inhibit food consumption increased by 10 ug icv infusion of NPY followed by compound administered at 10 mg/kg (ip) in satiated rats2002Bioorganic & medicinal chemistry letters, Feb-11, Volume: 12, Issue:3
Dihydropyridine neuropeptide Y Y(1) receptor antagonists.
AID146576Ability to inhibit human Neuropeptide Y1 receptor evaluated via forskolin-stimulated c-AMP accumulation in chinese hamster (CHO) cells2002Bioorganic & medicinal chemistry letters, Feb-11, Volume: 12, Issue:3
Dihydropyridine neuropeptide Y Y(1) receptor antagonists.
AID146603Binding affinity for human Neuropeptide Y2 receptor; No affinity2002Bioorganic & medicinal chemistry letters, Feb-11, Volume: 12, Issue:3
Dihydropyridine neuropeptide Y Y(1) receptor antagonists.
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 (18)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's4 (22.22)29.6817
2010's9 (50.00)24.3611
2020's5 (27.78)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 17.77

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 Index17.77 (24.57)
Research Supply Index2.48 (2.92)
Research Growth Index5.08 (4.65)
Search Engine Demand Index10.37 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (17.77)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Observational0 (0.00%)0.25%
Other11 (100.00%)84.16%
Other8 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]