Page last updated: 2024-12-11

pd 136450

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

Description

PD 136450: gastrin receptor antagonist; dipeptoid which resembles the carboxy-terminal moiety of gastrin [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID6439414
CHEMBL ID341460
CHEMBL ID3351022
SCHEMBL ID6895211
MeSH IDM0208408

Synonyms (22)

Synonym
2-butenoic acid, 4-((2-((3-(1h-indol-3-yl)-2-methyl-1-oxo-2-(((tricyclo(3.3.1.1(3,7))dec-2-yloxy)carbonyl)amino)propyl)amino)-1-phenylethyl)amino)-4-oxo-, (r-(r*,r*))-
gtpl867
pd-136,450
139067-52-0
cam-1189
cam 1189
pd-136450
4-((2- ((3-(1h-indol-3-yl)-2-methyl-1-oxo-2-(((tricyclo(3.3.1.1(3,7))dec-2-yloxy)carbonyl)amino)propyl)amino)-1-phenylethyl)amino)-4-oxo-2-butenoic acid
pd136450 ,
cam1189
pd 136450
CHEMBL341460 ,
bdbm50007439
3-{2-[2-(adamantan-2-yloxycarbonylamino)-3-(1h-indol-3-yl)-2-methyl-propionylamino]-1-phenyl-ethylcarbamoyl}-acrylic acid
(e)-4-[[(1r)-2-[[(2r)-2-(2-adamantyloxycarbonylamino)-3-(1h-indol-3-yl)-2-methylpropanoyl]amino]-1-phenylethyl]amino]-4-oxobut-2-enoic acid
SCHEMBL6895211
CHEMBL3351022 ,
Q27088262
bdbm50230677
(e)-4-[[2-[[2-(2-adamantyloxycarbonylamino)-3-(1h-indol-3-yl)-2-methylpropanoyl]amino]-1-phenylethyl]amino]-4-oxobut-2-enoic acid
2-butenoic acid, 4-[[(1r)-2-[[(2r)-3-(1h-indol-3-yl)-2-methyl-1-oxo-2-[[(tricyclo[3.3.1.13,7]dec-2-yloxy)carbonyl]amino]propyl]amino]-1-phenylethyl]amino]-4-oxo-
AKOS040749145

Research Excerpts

Dosage Studied

ExcerptRelevanceReference
" Increasing concentrations of PD 136450 caused a monophasic dose-response curve in contrast to the well-known biphasic amylase release in response to CCK8."( A new CCK-B/gastrin receptor antagonist acts as an agonist on the rat pancreas.
Arnold, R; Eissele, R; Koop, H; Koop, I; Meyer, F; Mössner, J; Patberg, H; Richter, S, 1994
)
0.58
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (1)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Cholecystokinin receptor type ARattus norvegicus (Norway rat)IC50 (µMol)0.79000.00000.43624.3000AID53030
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (7)

Assay IDTitleYearJournalArticle
AID51119Half-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to mouse cerebral cortex Cholecystokinin type B receptor1991Journal of medicinal chemistry, Jan, Volume: 34, Issue:1
Rationally designed "dipeptoid" analogues of CCK. alpha-Methyltryptophan derivatives as highly selective and orally active gastrin and CCK-B antagonists with potent anxiolytic properties.
AID50513Ratio calculated as IC50 ratio of Cholecystokinin type A receptor to that of Cholecystokinin type B receptor1991Journal of medicinal chemistry, Jan, Volume: 34, Issue:1
Rationally designed "dipeptoid" analogues of CCK. alpha-Methyltryptophan derivatives as highly selective and orally active gastrin and CCK-B antagonists with potent anxiolytic properties.
AID178584Effective dose to inhibit pentagastrin stimulated gastric acid secretion in rats(iv administration)1991Journal of medicinal chemistry, Jan, Volume: 34, Issue:1
Rationally designed "dipeptoid" analogues of CCK. alpha-Methyltryptophan derivatives as highly selective and orally active gastrin and CCK-B antagonists with potent anxiolytic properties.
AID178585Effective dose to inhibit pentagastrin stimulated gastric acid secretion in rats(sc administration)1991Journal of medicinal chemistry, Jan, Volume: 34, Issue:1
Rationally designed "dipeptoid" analogues of CCK. alpha-Methyltryptophan derivatives as highly selective and orally active gastrin and CCK-B antagonists with potent anxiolytic properties.
AID53030Half-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas Cholecystokinin type A receptor1991Journal of medicinal chemistry, Jan, Volume: 34, Issue:1
Rationally designed "dipeptoid" analogues of CCK. alpha-Methyltryptophan derivatives as highly selective and orally active gastrin and CCK-B antagonists with potent anxiolytic properties.
AID51280Cholecystokinin type B receptor binding assay performed on homogenized cerebral cortex from male mouse1992Journal of medicinal chemistry, May-01, Volume: 35, Issue:9
Rationally designed "dipeptoid" analogues of CCK. A Free-Wilson/Fujita-Ban analysis of some alpha-methyltryptophan derivatives as CCK-B antagonists.
AID1346809Rat CCK1 receptor (Cholecystokinin receptors)1994The Journal of pharmacology and experimental therapeutics, Jun, Volume: 269, Issue:3
Characterization of cholecystokininA receptor agonist activity by a family of cholecystokininB receptor antagonists.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (13)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's10 (76.92)18.2507
2000's2 (15.38)29.6817
2010's1 (7.69)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: 11.50

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 Index11.50 (24.57)
Research Supply Index2.71 (2.92)
Research Growth Index4.20 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.50)

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%
Other14 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]