Compounds > pd 176252
Page last updated: 2024-12-11

pd 176252

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Description

PD 176252: a non-peptide gastrin-releasing peptide (BB2) receptor antagonist; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID9829828
CHEMBL ID405908
SCHEMBL ID397897
MeSH IDM0300057

Synonyms (30)

Synonym
CHEMBL405908 ,
pd-176252
(2s)-3-(1h-indol-3-yl)-n-[[1-(5-methoxypyridin-2-yl)cyclohexyl]methyl]-2-methyl-2-[(4-nitrophenyl)carbamoylamino]propanamide
gtpl626
pd 176252
bdbm50071739
(s)-3-(1h-indol-3-yl)-n-[1-(5-methoxy-pyridin-2-yl)-cyclohexylmethyl]-2-methyl-2-[3-(4-nitro-phenyl)-ureido]-propionamide
(s)-n-[[1-(5-methoxy-2-pyridinyl)cyclohexyl]methyl]-a-methyl-a-[[-(4-nitrophenyl)amino]carbonyl]amino-1h-indole-3-propanamide
204067-01-6
1h-indole-3-propanamide, n-((1-(5-methoxy-2-pyridinyl)cyclohexyl)methyl)-.alpha.-methyl-.alpha.-((((4-nitrophenyl)amino)carbonyl)amino)-, (s)-
1h-indole-3-propanamide, n-((1-(5-methoxy-2-pyridinyl)cyclohexyl)methyl)-.alpha.-methyl-.alpha.-((((4-nitrophenyl)amino)carbonyl)amino)-, (.alpha.s)-
JT21Y57650 ,
1h-indole-3-propanamide, n-((1-(5-methoxy-2-pyridinyl)cyclohexyl)methyl)-alpha-methyl-alpha-((((4-nitrophenyl)amino)carbonyl)amino)-, (s)-
pd176252 ,
unii-jt21y57650
1h-indole-3-propanamide, n-((1-(5-methoxy-2-pyridinyl)cyclohexyl)methyl)-alpha-methyl-alpha-((((4-nitrophenyl)amino)carbonyl)amino)-, (alphas)-
SCHEMBL397897
(s)-n-[[1-(5-methoxy-2-pyridinyl)cyclohexyl]methyl]-?-methyl-?-[[[-(4-nitrophenyl)amino]carbonyl]amino-1h-indole-3-propanamide
AKOS024457189
DTXSID90431389
J-013286
NCGC00378666-01
Q27088279
HY-103286
CS-0027145
HMS3742I15
(s)-n-[[1-(5-methoxy-2-pyridinyl)cyclohexyl]methyl]-alpha-methyl-alpha-[[[-(4-nitrophenyl)amino]carbonyl]amino-1h-indole-3-propanamide
MS-30465
8B8 ,
AKOS040742374

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 (9)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency0.95220.01237.983543.2770AID1645841
GVesicular stomatitis virusPotency2.68370.01238.964839.8107AID1645842
cytochrome P450 2D6Homo sapiens (human)Potency3.01120.00108.379861.1304AID1645840
Interferon betaHomo sapiens (human)Potency2.68370.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency2.68370.01238.964839.8107AID1645842
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency2.68370.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency2.68370.01238.964839.8107AID1645842
[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)
Neuromedin-B receptorHomo sapiens (human)Ki0.00020.00020.00080.0020AID42490
Gastrin-releasing peptide receptorHomo sapiens (human)Ki0.00100.00020.00610.0170AID42631
[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)
Neuromedin-B receptorHomo sapiens (human)KB app0.00320.00230.00320.0040AID42491; AID42492
Gastrin-releasing peptide receptorHomo sapiens (human)KB app0.02450.01300.02450.0360AID42632; AID42633
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (62)

Processvia Protein(s)Taxonomy
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
positive regulation of T cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
adaptive immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-independentHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of T cell anergyHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
defense responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
detection of bacteriumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-12 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-6 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protection from natural killer cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
innate immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of dendritic cell differentiationHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class IbHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayNeuromedin-B receptorHomo sapiens (human)
neuropeptide signaling pathwayNeuromedin-B receptorHomo sapiens (human)
bombesin receptor signaling pathwayNeuromedin-B receptorHomo sapiens (human)
negative regulation of interleukin-6 productionNeuromedin-B receptorHomo sapiens (human)
positive regulation of interferon-alpha productionNeuromedin-B receptorHomo sapiens (human)
positive regulation of osteoclast proliferationNeuromedin-B receptorHomo sapiens (human)
antiviral innate immune responseNeuromedin-B receptorHomo sapiens (human)
sneeze reflexNeuromedin-B receptorHomo sapiens (human)
positive regulation of respiratory gaseous exchangeNeuromedin-B receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayNeuromedin-B receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayGastrin-releasing peptide receptorHomo sapiens (human)
neuropeptide signaling pathwayGastrin-releasing peptide receptorHomo sapiens (human)
learning or memoryGastrin-releasing peptide receptorHomo sapiens (human)
social behaviorGastrin-releasing peptide receptorHomo sapiens (human)
psychomotor behaviorGastrin-releasing peptide receptorHomo sapiens (human)
regulation of cell population proliferationGastrin-releasing peptide receptorHomo sapiens (human)
response to external biotic stimulusGastrin-releasing peptide receptorHomo sapiens (human)
motor behaviorGastrin-releasing peptide receptorHomo sapiens (human)
positive regulation of respiratory gaseous exchangeGastrin-releasing peptide receptorHomo sapiens (human)
positive regulation of behavioral fear responseGastrin-releasing peptide receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayGastrin-releasing peptide receptorHomo sapiens (human)
inositol phosphate metabolic processInositol hexakisphosphate kinase 1Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
negative regulation of cold-induced thermogenesisInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (22)

Processvia Protein(s)Taxonomy
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
signaling receptor bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
peptide antigen bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein-folding chaperone bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
bombesin receptor activityNeuromedin-B receptorHomo sapiens (human)
neuropeptide receptor activityNeuromedin-B receptorHomo sapiens (human)
neuropeptide receptor activityGastrin-releasing peptide receptorHomo sapiens (human)
G protein-coupled peptide receptor activityGastrin-releasing peptide receptorHomo sapiens (human)
neuropeptide bindingGastrin-releasing peptide receptorHomo sapiens (human)
inositol-1,3,4,5,6-pentakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol heptakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
ATP bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 1-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 3-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (22)

Processvia Protein(s)Taxonomy
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
Golgi membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
endoplasmic reticulumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
Golgi apparatusHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
cell surfaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
ER to Golgi transport vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
secretory granule membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
phagocytic vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
early endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
recycling endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular exosomeHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
lumenal side of endoplasmic reticulum membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
MHC class I protein complexHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular spaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
external side of plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
cytosolNeuromedin-B receptorHomo sapiens (human)
plasma membraneNeuromedin-B receptorHomo sapiens (human)
plasma membraneNeuromedin-B receptorHomo sapiens (human)
plasma membraneGastrin-releasing peptide receptorHomo sapiens (human)
plasma membraneGastrin-releasing peptide receptorHomo sapiens (human)
fibrillar centerInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
cytosolInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleusInositol hexakisphosphate kinase 1Homo sapiens (human)
cytoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (27)

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.
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.
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.
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.
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.
AID1575576Antiinflammatory activity in human HK2 cells assessed as suppression of cisplatin-induced TNF-alpha mRNA level at 4 uM by SYBR-green based RT-PCR analysis2019MedChemComm, May-01, Volume: 10, Issue:5
Design, synthesis and evaluation of PD176252 analogues for ameliorating cisplatin-induced nephrotoxicity.
AID42632In vitro inhibition of acidification responses to NMC at the human Bombesin receptor bb2 expressed in CHO cells; 2-281998Bioorganic & medicinal chemistry letters, Sep-22, Volume: 8, Issue:18
PD 176252--the first high affinity non-peptide gastrin-releasing peptide (BB2) receptor antagonist.
AID1575583Induction of NF-kappaB p65 phosphorylation in human HK2 cells at 4 uM by Western blot analysis2019MedChemComm, May-01, Volume: 10, Issue:5
Design, synthesis and evaluation of PD176252 analogues for ameliorating cisplatin-induced nephrotoxicity.
AID1575574Cytotoxicity against human HK2 cells assessed as reduction in cell viability after 24 hrs by MTT assay2019MedChemComm, May-01, Volume: 10, Issue:5
Design, synthesis and evaluation of PD176252 analogues for ameliorating cisplatin-induced nephrotoxicity.
AID1575582Inhibition of cisplatin-induced NF-kappaB p65 phosphorylation in human HK2 cells at 4 uM by Western blot analysis2019MedChemComm, May-01, Volume: 10, Issue:5
Design, synthesis and evaluation of PD176252 analogues for ameliorating cisplatin-induced nephrotoxicity.
AID42633In vitro inhibition of bombesin-evoked increases in intracellular calcium level in CHO cells stably expressed human Bombesin receptor bb2; 14-941998Bioorganic & medicinal chemistry letters, Sep-22, Volume: 8, Issue:18
PD 176252--the first high affinity non-peptide gastrin-releasing peptide (BB2) receptor antagonist.
AID1575577Antiinflammatory activity in human HK2 cells assessed as suppression of cisplatin-induced IL-6 mRNA level at 4 uM by SYBR-green based RT-PCR analysis2019MedChemComm, May-01, Volume: 10, Issue:5
Design, synthesis and evaluation of PD176252 analogues for ameliorating cisplatin-induced nephrotoxicity.
AID42492In vitro inhibition of bombesin-evoked increases in intracellular calcium level in CHO cells stably expressed human Bombesin receptor bb1; 1-6.61998Bioorganic & medicinal chemistry letters, Sep-22, Volume: 8, Issue:18
PD 176252--the first high affinity non-peptide gastrin-releasing peptide (BB2) receptor antagonist.
AID1575580Antiinflammatory activity in human HK2 cells assessed as suppression of cisplatin-induced IL-6 mRNA level at 4 uM by ELISA2019MedChemComm, May-01, Volume: 10, Issue:5
Design, synthesis and evaluation of PD176252 analogues for ameliorating cisplatin-induced nephrotoxicity.
AID1575579Antiinflammatory activity in human HK2 cells assessed as suppression of cisplatin-induced TNF-alpha mRNA level at 4 uM by ELISA2019MedChemComm, May-01, Volume: 10, Issue:5
Design, synthesis and evaluation of PD176252 analogues for ameliorating cisplatin-induced nephrotoxicity.
AID1575578Antiinflammatory activity in human HK2 cells assessed as suppression of cisplatin-induced MCP-1 mRNA level at 4 uM by SYBR-green based RT-PCR analysis2019MedChemComm, May-01, Volume: 10, Issue:5
Design, synthesis and evaluation of PD176252 analogues for ameliorating cisplatin-induced nephrotoxicity.
AID1232214Half life in rat liver microsomes at 1 uM preincubated for 10 mins followed by addition of NADPH regenerating system by LC-MS analysis2015Bioorganic & medicinal chemistry, Jul-15, Volume: 23, Issue:14
Novel 3-(1H-indol-3-yl)-2-[3-(4-methoxyphenyl)ureido]propanamides as selective agonists of human formyl-peptide receptor 2.
AID1575581Antiinflammatory activity in human HK2 cells assessed as suppression of cisplatin-induced MCP-1 mRNA level at 4 uM by ELISA2019MedChemComm, May-01, Volume: 10, Issue:5
Design, synthesis and evaluation of PD176252 analogues for ameliorating cisplatin-induced nephrotoxicity.
AID42491In vitro inhibition of acidification responses to NMB at the human Bombesin receptor bb1 expressed in CHO cells; 1-171998Bioorganic & medicinal chemistry letters, Sep-22, Volume: 8, Issue:18
PD 176252--the first high affinity non-peptide gastrin-releasing peptide (BB2) receptor antagonist.
AID42631Antagonistic activity against cloned human Bombesin receptor bb2 labeled with [125I]- [Tyr] bombesin stably expressed in CHO cells; 0.66-1.31998Bioorganic & medicinal chemistry letters, Sep-22, Volume: 8, Issue:18
PD 176252--the first high affinity non-peptide gastrin-releasing peptide (BB2) receptor antagonist.
AID1232215Intrinsic clearance in rat liver microsomes at 1 uM preincubated for 10 mins followed by addition of NADPH regenerating system by LC-MS analysis2015Bioorganic & medicinal chemistry, Jul-15, Volume: 23, Issue:14
Novel 3-(1H-indol-3-yl)-2-[3-(4-methoxyphenyl)ureido]propanamides as selective agonists of human formyl-peptide receptor 2.
AID42489Antagonistic activity against labelled Bombesin receptor bb1 binding sites in rat olfactory bulb by using [125I]- [Tyr] bombesin in presence of [D-Phe-6] bombesin(6-13)ethyl ester; 0.31-1.31998Bioorganic & medicinal chemistry letters, Sep-22, Volume: 8, Issue:18
PD 176252--the first high affinity non-peptide gastrin-releasing peptide (BB2) receptor antagonist.
AID42490Antagonism of recombinant human bombesin receptor (bb1) labeled with [125I]- [Tyr] bombesin stably expressed in CHO cells1998Bioorganic & medicinal chemistry letters, Sep-22, Volume: 8, Issue:18
PD 176252--the first high affinity non-peptide gastrin-releasing peptide (BB2) receptor antagonist.
AID42629Antagonistic activity against labelled Bombesin receptor bb2 binding sites in rat cerebral cortex by using [125I]- [Tyr] bombesin in presence of NMB; 6.5-311998Bioorganic & medicinal chemistry letters, Sep-22, Volume: 8, Issue:18
PD 176252--the first high affinity non-peptide gastrin-releasing peptide (BB2) receptor antagonist.
AID1346539Human BB2 receptor (Bombesin receptors)1998Bioorganic & medicinal chemistry letters, Sep-22, Volume: 8, Issue:18
PD 176252--the first high affinity non-peptide gastrin-releasing peptide (BB2) receptor antagonist.
AID1346439Human BB1 receptor (Bombesin receptors)2009Peptides, Aug, Volume: 30, Issue:8
Characterization of putative GRP- and NMB-receptor antagonist's interaction with human receptors.
AID1346539Human BB2 receptor (Bombesin receptors)2009Peptides, Aug, Volume: 30, Issue:8
Characterization of putative GRP- and NMB-receptor antagonist's interaction with human receptors.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (22)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's1 (4.55)18.2507
2000's6 (27.27)29.6817
2010's12 (54.55)24.3611
2020's3 (13.64)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 11.88

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 Index11.88 (24.57)
Research Supply Index3.14 (2.92)
Research Growth Index5.02 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.88)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (4.55%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other21 (95.45%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
diclofenac
Diclofenac: A non-steroidal anti-inflammatory agent (NSAID) with antipyretic and analgesic actions. It is primarily available as the sodium salt.. diclofenac : A monocarboxylic acid consisting of phenylacetic acid having a (2,6-dichlorophenyl)amino group at the 2-position.		2.1110amino acid;
aromatic amine;
dichlorobenzene;
monocarboxylic acid;
secondary amino compound		antipyretic;
drug allergen;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
environmental contaminant;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
xenobiotic
entinostat
[no description available]		2.0310benzamides;
carbamate ester;
primary amino compound;
pyridines;
substituted aniline		antineoplastic agent;
apoptosis inducer;
EC 3.5.1.98 (histone deacetylase) inhibitor
pd 153035
4-((3-bromophenyl)amino)-6,7-dimethoxyquinazoline: structure given in first source. PD-153035 : A member of the class of quinazolines carrying a 3-bromophenylamino substituent at position 4 and two methoxy substituents at positions 6 and 7.		2.0510aromatic amine;
aromatic ether;
bromobenzenes;
quinazolines;
secondary amino compound		EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
epidermal growth factor receptor antagonist
potassium chloride
Potassium Chloride: A white crystal or crystalline powder used in BUFFERS; FERTILIZERS; and EXPLOSIVES. It can be used to replenish ELECTROLYTES and restore WATER-ELECTROLYTE BALANCE in treating HYPOKALEMIA.. potassium chloride : A metal chloride salt with a K(+) counterion.		2.0710inorganic chloride;
inorganic potassium salt;
potassium salt		fertilizer
propafenone
Propafenone: An antiarrhythmia agent that is particularly effective in ventricular arrhythmias. It also has weak beta-blocking activity.. propafenone : An aromatic ketone that is 3-(propylamino)propane-1,2-diol in which the hydrogen of the primary hydroxy group is replaced by a 2-(3-phenylpropanoyl)phenyl group. It is a class 1C antiarrhythmic drug with local anesthetic effects, and is used as the hydrochloride salt in the management of supraventricular and ventricular arrhythmias.		2.1110aromatic ketone;
secondary alcohol;
secondary amino compound		anti-arrhythmia drug
tryptophan
Tryptophan: An essential amino acid that is necessary for normal growth in infants and for NITROGEN balance in adults. It is a precursor of INDOLE ALKALOIDS in plants. It is a precursor of SEROTONIN (hence its use as an antidepressant and sleep aid). It can be a precursor to NIACIN, albeit inefficiently, in mammals.. tryptophan : An alpha-amino acid that is alanine bearing an indol-3-yl substituent at position 3.		2.1510erythrose 4-phosphate/phosphoenolpyruvate family amino acid;
L-alpha-amino acid zwitterion;
L-alpha-amino acid;
proteinogenic amino acid;
tryptophan zwitterion;
tryptophan		antidepressant;
Escherichia coli metabolite;
human metabolite;
micronutrient;
mouse metabolite;
nutraceutical;
plant metabolite;
Saccharomyces cerevisiae metabolite
quinoxalines
quinoxaline : A naphthyridine in which the nitrogens are at positions 1 and 4.		2.1110mancude organic heterobicyclic parent;
naphthyridine;
ortho-fused heteroarene
quinazolines
Quinazolines: A group of aromatic heterocyclic compounds that contain a bicyclic structure with two fused six-membered aromatic rings, a benzene ring and a pyrimidine ring.. quinazoline : A mancude organic heterobicyclic parent that is naphthalene in which the carbon atoms at positions 1 and 3 have been replaced by nitrogen atoms.. quinazolines : Any organic heterobicyclic compound based on a quinazoline skeleton and its substituted derivatives.		2.4520azaarene;
mancude organic heterobicyclic parent;
ortho-fused heteroarene;
quinazolines
p-methoxy-n-methylphenethylamine
p-Methoxy-N-methylphenethylamine: A potent mast cell degranulator. It is involved in histamine release.. N,O-dimethyltyramine : A secondary amino compound that is tyramine in which the hydrogen of the phenolic hydroxy group has been replaced by a methyl group.		2.1110aromatic ether;
secondary amino compound		metabolite
rc 3095
bombesin (6-14), Tpi(6)-Leu(13)-psi(CH2NH)-Leu(14)-: an antagonist of bombesin		3.8930
erlotinib hydrochloride
[no description available]		2.0310hydrochloride;
terminal acetylenic compound		antineoplastic agent;
protein kinase inhibitor
oxytocin
Oxytocin: A nonapeptide hormone released from the neurohypophysis (PITUITARY GLAND, POSTERIOR). It differs from VASOPRESSIN by two amino acids at residues 3 and 8. Oxytocin acts on SMOOTH MUSCLE CELLS, such as causing UTERINE CONTRACTIONS and MILK EJECTION.. oxytocin : A cyclic nonapeptide hormone with amino acid sequence CYIQNCPLG that also acts as a neurotransmitter in the brain; the principal uterine-contracting and milk-ejecting hormone of the posterior pituitary. Together with the neuropeptide vasopressin, it is believed to influence social cognition and behaviour.		2.0710heterodetic cyclic peptide;
peptide hormone		oxytocic;
vasodilator agent
capsaicin
ALGRX-4975: an injectable capsaicin (TRPV1 receptor agonist) formulation for longlasting pain relief. capsaicinoid : A family of aromatic fatty amides produced as secondary metabolites by chilli peppers.		2.1110capsaicinoidnon-narcotic analgesic;
TRPV1 agonist;
voltage-gated sodium channel blocker
mtt formazan
MTT formazan: a blue MEM-insoluble mitochondrial byproduct; used to determine viability of cells with active mitochondrial dehydrogenase enzymes		2.0310
as 605240
5-quinoxalin-6-ylmethylenethiazolidine-2,4-dione: a PI3Kgamma inhibitor; structure in first source. (5Z)-5-(quinoxalin-6-ylmethylidene)-1,3-thiazolidine-2,4-dione : A quinoxaline derivative that is quinoxaline in which the hydrogen at position 6 is replaced by a (2,4-dioxo-1,3-thiazolidin-5-ylidene)methyl group. It is a potent inhibitor of the PI3Kgamma, with an IC50 of 8 nM and inhibits the progression of joint inflammation and damage in both lymphocyte-independent and dependent mouse models of rheumatoid arthritis.		2.1110quinoxaline derivative;
thiazolidinediones		anti-inflammatory agent;
antirheumatic drug;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor
neurokinin b
Neurokinin B: A mammalian neuropeptide of 10 amino acids that belongs to the tachykinin family. It is similar in structure and action to SUBSTANCE P and NEUROKININ A with the ability to excite neurons, dilate blood vessels, and contract smooth muscles, such as those in the URINARY BLADDER and UTERUS.		2.420polypeptide
formazans
Formazans: Colored azo compounds formed by the reduction of tetrazolium salts. Employing this reaction, oxidoreductase activity can be determined quantitatively in tissue sections by allowing the enzymes to act on their specific substrates in the presence of tetrazolium salts.		2.0310
pd 168368
PD 168368: a neuromedin B receptor antagonist; structure in first source		3.2860
oxadiazoles
Oxadiazoles: Compounds containing five-membered heteroaromatic rings containing two carbons, two nitrogens, and one oxygen atom which exist in various regioisomeric forms.		2.4110
bombesin
[no description available]		1.9910
neuromedin b
neuromedin B: decapeptide isolated from porcine spinal cord		2.420
gastrin-releasing peptide
Gastrin-Releasing Peptide: Neuropeptide and gut hormone that helps regulate GASTRIC ACID secretion and motor function. Once released from nerves in the antrum of the STOMACH, the neuropeptide stimulates release of GASTRIN from the GASTRIN-SECRETING CELLS.		9.4160
ConditionIndicatedRelationship StrengthStudiesTrials
Congenital Zika Syndrome
[description not available]		02.2510
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		02.5720
Zika Virus Infection
A viral disease transmitted by the bite of AEDES mosquitoes infected with ZIKA VIRUS. Its mild DENGUE-like symptoms include fever, rash, headaches and ARTHRALGIA. The viral infection during pregnancy, in rare cases, is associated with congenital brain and ocular abnormalities, called Congenital Zika Syndrome, including MICROCEPHALY and may also lead to GUILLAIN-BARRE SYNDROME.		02.2510
Benign Neoplasms
[description not available]		03.5320
Neoplasms
New abnormal growth of tissue. Malignant neoplasms show a greater degree of anaplasia and have the properties of invasion and metastasis, compared to benign neoplasms.		03.5320
Itching
[description not available]		02.5520
Pruritus
An intense itching sensation that produces the urge to rub or scratch the skin to obtain relief.		02.5520
Hepatocellular Carcinoma
[description not available]		02.0510
Cancer of Liver
[description not available]		02.0510
Carcinoma, Hepatocellular
A primary malignant neoplasm of epithelial liver cells. It ranges from a well-differentiated tumor with EPITHELIAL CELLS indistinguishable from normal HEPATOCYTES to a poorly differentiated neoplasm. The cells may be uniform or markedly pleomorphic, or form GIANT CELLS. Several classification schemes have been suggested.		02.0510
Liver Neoplasms
Tumors or cancer of the LIVER.		02.0510
Preterm Birth
[description not available]		02.0710
Pregnancy
The status during which female mammals carry their developing young (EMBRYOS or FETUSES) in utero before birth, beginning from FERTILIZATION to BIRTH.		02.0710
Premature Birth
CHILDBIRTH before 37 weeks of PREGNANCY (259 days from the first day of the mother's last menstrual period, or 245 days after FERTILIZATION).		02.0710
Cancer of Lung
[description not available]		02.4220
Lung Neoplasms
Tumors or cancer of the LUNG.		02.4220
Anxiety
Feelings or emotions of dread, apprehension, and impending disaster but not disabling as with ANXIETY DISORDERS.		02.0310
Cancer of Head
[description not available]		02.0310
Invasiveness, Neoplasm
[description not available]		02.0310
Head and Neck Neoplasms
Soft tissue tumors or cancer arising from the mucosal surfaces of the LIP; oral cavity; PHARYNX; LARYNX; and cervical esophagus. Other sites included are the NOSE and PARANASAL SINUSES; SALIVARY GLANDS; THYROID GLAND and PARATHYROID GLANDS; and MELANOMA and non-melanoma skin cancers of the head and neck. (from Holland et al., Cancer Medicine, 4th ed, p1651)		02.0310