Page last updated: 2024-12-11

pd 154075

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

Description

PD 154075: a non-peptide tachykinin NK1 receptor antagonist; structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID9805809
CHEMBL ID307488
SCHEMBL ID2139814
MeSH IDM0237092

Synonyms (17)

Synonym
pd-154075
CHEMBL307488 ,
[(r)-2-(3h-indol-3-yl)-1-methyl-1-((s)-1-phenyl-ethylcarbamoyl)-ethyl]-carbamic acid benzofuran-2-ylmethyl ester
bdbm50101416
[2-(1h-indol-3-yl)-1-methyl-1-(1-phenyl-ethylcarbamoyl)-ethyl]-carbamic acid benzofuran-2-ylmethyl ester
SCHEMBL2139814
unii-qk6iajla0m
2-benzofuranylmethoxycarbonyl-alpha-methyltryptophan-n-(1-phenylethyl)amide
pd 154075
ci-1021
158991-23-2
1-benzofuran-2-ylmethyl (1r)-1-(1h-indol-3-ylmethyl)-1-methyl-2-oxo-2-[[(1s)-1-phenylethyl]amino]ethylcarbamate
QK6IAJLA0M ,
carbamic acid, n-((1r)-1-(1h-indol-3-ylmethyl)-1-methyl-2-oxo-2-(((1s)-1-phenylethyl)amino)ethyl)-, 2-benzofuranylmethyl ester
DTXSID201107758
2-benzofuranylmethyl n-[(1r)-1-(1h-indol-3-ylmethyl)-1-methyl-2-oxo-2-[[(1s)-1-phenylethyl]amino]ethyl]carbamate
carbamic acid, n-[(1r)-1-(1h-indol-3-ylmethyl)-1-methyl-2-oxo-2-[[(1s)-1-phenylethyl]amino]ethyl]-, 2-benzofuranylmethyl ester
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (2)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Substance-P receptorHomo sapiens (human)IC50 (µMol)0.00210.00000.09526.8130AID1202705; AID208094; AID208428; AID208589
Substance-P receptorCavia porcellus (domestic guinea pig)IC50 (µMol)0.00590.00002.751810.0000AID208094
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (38)

Processvia Protein(s)Taxonomy
aggressive behaviorSubstance-P receptorHomo sapiens (human)
positive regulation of leukocyte migrationSubstance-P receptorHomo sapiens (human)
angiotensin-mediated drinking behaviorSubstance-P receptorHomo sapiens (human)
inflammatory responseSubstance-P receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwaySubstance-P receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationSubstance-P receptorHomo sapiens (human)
tachykinin receptor signaling pathwaySubstance-P receptorHomo sapiens (human)
long-term memorySubstance-P receptorHomo sapiens (human)
associative learningSubstance-P receptorHomo sapiens (human)
detection of abiotic stimulusSubstance-P receptorHomo sapiens (human)
response to ozoneSubstance-P receptorHomo sapiens (human)
positive regulation of epithelial cell migrationSubstance-P receptorHomo sapiens (human)
response to auditory stimulusSubstance-P receptorHomo sapiens (human)
regulation of smooth muscle cell migrationSubstance-P receptorHomo sapiens (human)
positive regulation of synaptic transmission, cholinergicSubstance-P receptorHomo sapiens (human)
positive regulation of synaptic transmission, GABAergicSubstance-P receptorHomo sapiens (human)
response to estradiolSubstance-P receptorHomo sapiens (human)
response to progesteroneSubstance-P receptorHomo sapiens (human)
response to nicotineSubstance-P receptorHomo sapiens (human)
operant conditioningSubstance-P receptorHomo sapiens (human)
sperm ejaculationSubstance-P receptorHomo sapiens (human)
eating behaviorSubstance-P receptorHomo sapiens (human)
positive regulation of vascular permeabilitySubstance-P receptorHomo sapiens (human)
response to ethanolSubstance-P receptorHomo sapiens (human)
positive regulation of action potentialSubstance-P receptorHomo sapiens (human)
positive regulation of blood pressureSubstance-P receptorHomo sapiens (human)
positive regulation of ossificationSubstance-P receptorHomo sapiens (human)
positive regulation of vasoconstrictionSubstance-P receptorHomo sapiens (human)
positive regulation of hormone secretionSubstance-P receptorHomo sapiens (human)
behavioral response to painSubstance-P receptorHomo sapiens (human)
regulation of smooth muscle cell proliferationSubstance-P receptorHomo sapiens (human)
positive regulation of lymphocyte proliferationSubstance-P receptorHomo sapiens (human)
positive regulation of epithelial cell proliferationSubstance-P receptorHomo sapiens (human)
positive regulation of stress fiber assemblySubstance-P receptorHomo sapiens (human)
response to electrical stimulusSubstance-P receptorHomo sapiens (human)
smooth muscle contraction involved in micturitionSubstance-P receptorHomo sapiens (human)
positive regulation of uterine smooth muscle contractionSubstance-P receptorHomo sapiens (human)
positive regulation of flagellated sperm motilitySubstance-P receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (3)

Processvia Protein(s)Taxonomy
tachykinin receptor activitySubstance-P receptorHomo sapiens (human)
protein bindingSubstance-P receptorHomo sapiens (human)
substance P receptor activitySubstance-P receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (7)

Processvia Protein(s)Taxonomy
plasma membraneSubstance-P receptorHomo sapiens (human)
cell surfaceSubstance-P receptorHomo sapiens (human)
dendriteSubstance-P receptorHomo sapiens (human)
sperm flagellumSubstance-P receptorHomo sapiens (human)
cell bodySubstance-P receptorHomo sapiens (human)
sperm headSubstance-P receptorHomo sapiens (human)
sperm midpieceSubstance-P receptorHomo sapiens (human)
plasma membraneSubstance-P receptorHomo sapiens (human)
sperm midpieceSubstance-P receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (11)

Assay IDTitleYearJournalArticle
AID1202707Antagonist activity at NK1 receptor in substance P-induced gerbil foot tapping model2015Journal of medicinal chemistry, Mar-26, Volume: 58, Issue:6
CNS drug design: balancing physicochemical properties for optimal brain exposure.
AID1202706AUC (0 to 1 hr) in rat at 0.5 mg/kg, iv2015Journal of medicinal chemistry, Mar-26, Volume: 58, Issue:6
CNS drug design: balancing physicochemical properties for optimal brain exposure.
AID1202704Solubility of the compound2015Journal of medicinal chemistry, Mar-26, Volume: 58, Issue:6
CNS drug design: balancing physicochemical properties for optimal brain exposure.
AID1202702Oral bioavailability in dog2015Journal of medicinal chemistry, Mar-26, Volume: 58, Issue:6
CNS drug design: balancing physicochemical properties for optimal brain exposure.
AID208428Inhibition of specific binding at tachykinin receptor 12001Journal of medicinal chemistry, Jul-05, Volume: 44, Issue:14
Utilization of an intramolecular hydrogen bond to increase the CNS penetration of an NK(1) receptor antagonist.
AID21526Solubility in water was determined2000Bioorganic & medicinal chemistry letters, May-15, Volume: 10, Issue:10
Phosphate prodrugs of PD154075.
AID208589Binding affinity towards tachykinin receptor 1 in human IM9 cells.1995Journal of medicinal chemistry, Oct-27, Volume: 38, Issue:22
Quantitative structure-activity relationships (QSARs) of N-terminus fragments of NK1 tachykinin antagonists: a comparison of classical QSARs and three-dimensional QSARs from similarity matrices.
AID208094In vitro affinity for specific binding at Gerbil tachykinin receptor 12001Journal of medicinal chemistry, Jul-05, Volume: 44, Issue:14
Utilization of an intramolecular hydrogen bond to increase the CNS penetration of an NK(1) receptor antagonist.
AID1202694Ratio of drug uptake in brain to plasma in rat2015Journal of medicinal chemistry, Mar-26, Volume: 58, Issue:6
CNS drug design: balancing physicochemical properties for optimal brain exposure.
AID1202703Half life in dog2015Journal of medicinal chemistry, Mar-26, Volume: 58, Issue:6
CNS drug design: balancing physicochemical properties for optimal brain exposure.
AID1202705Antagonist activity at NK1 receptor (unknown origin)2015Journal of medicinal chemistry, Mar-26, Volume: 58, Issue:6
CNS drug design: balancing physicochemical properties for optimal brain exposure.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (8)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's5 (62.50)18.2507
2000's2 (25.00)29.6817
2010's1 (12.50)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.16

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 Index12.16 (24.57)
Research Supply Index2.20 (2.92)
Research Growth Index4.36 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.16)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews2 (25.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other6 (75.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]