Page last updated: 2024-12-08

h 142

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

Description

H 142: decapeptide inhibitor of human renin; RN given refers to all L-isomer [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID134897
CHEMBL ID407670
MeSH IDM0118469

Synonyms (15)

Synonym
u-76780e
CHEMBL407670 ,
l-lysine, n2-(n-(n-(n-(4-methyl-2-((n-(n-(1-(n-l-prolyl-l-histidyl)-l-prolyl)-l-phenylalanyl)-l-histidyl)amino)pentyl)-l-valyl)-l-isoleucyl)-l-histidyl)-, (s)-
h 142
85139-12-4
bdbm50022859
pro-his-prp-phe-his-leu(psi)[ch2nh]val-ile-his-lys
bdbm50022518
pro-his-pro-phe-his-leu[ch2nh]val-ile-his-lys
pro-his-prp-phe-his-leu(psi)[ch2nh]val-ile-his-lys(h-142)
pro-his-pro-phe-his-leu-ch2nh-val-ile-his-lys-oh
(2s)-6-amino-2-[[(2s)-3-(3h-imidazol-4-yl)-2-[[(2s,3s)-2-[[(2s)-2-[[(2s)-2-[[(2s)-3-(3h-imidazol-4-yl)-2-[[(2s)-2-[[(2s)-1-[(2s)-3-(3h-imidazol-4-yl)-2-[[(2s)-pyrrolidine-2-carbonyl]amino]propanoyl]pyrrolidine-2-carbonyl]amino]-3-phenyl-propanoyl]amino]pr
DTXSID40234281
((s)-2-((s)-2-((s)-2-((s)-1-(l-prolyl-l-histidyl)pyrrolidine-2-carboxamido)-3-phenylpropanamido)-3-(1h-imidazol-4-yl)propanamido)-4-methylpentyl)-l-valyl-l-isoleucyl-l-histidyl-l-lysine
AKOS040746879
[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)
ReninHomo sapiens (human)IC50 (µMol)0.00100.00000.77968.2000AID198663
Cathepsin D Bos taurus (cattle)IC50 (µMol)0.00700.00700.91656.3000AID47834
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
ReninHomo sapiens (human)Kd0.00800.00010.00410.0080AID198981
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (18)

Processvia Protein(s)Taxonomy
kidney developmentReninHomo sapiens (human)
mesonephros developmentReninHomo sapiens (human)
angiotensin maturationReninHomo sapiens (human)
renin-angiotensin regulation of aldosterone productionReninHomo sapiens (human)
proteolysisReninHomo sapiens (human)
regulation of blood pressureReninHomo sapiens (human)
male gonad developmentReninHomo sapiens (human)
hormone-mediated signaling pathwayReninHomo sapiens (human)
response to lipopolysaccharideReninHomo sapiens (human)
response to immobilization stressReninHomo sapiens (human)
drinking behaviorReninHomo sapiens (human)
regulation of MAPK cascadeReninHomo sapiens (human)
cell maturationReninHomo sapiens (human)
amyloid-beta metabolic processReninHomo sapiens (human)
response to cAMPReninHomo sapiens (human)
response to cGMPReninHomo sapiens (human)
cellular response to xenobiotic stimulusReninHomo sapiens (human)
juxtaglomerular apparatus developmentReninHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (5)

Processvia Protein(s)Taxonomy
aspartic-type endopeptidase activityReninHomo sapiens (human)
signaling receptor bindingReninHomo sapiens (human)
insulin-like growth factor receptor bindingReninHomo sapiens (human)
protein bindingReninHomo sapiens (human)
peptidase activityReninHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (6)

Processvia Protein(s)Taxonomy
extracellular regionReninHomo sapiens (human)
extracellular spaceReninHomo sapiens (human)
plasma membraneReninHomo sapiens (human)
apical part of cellReninHomo sapiens (human)
extracellular spaceReninHomo sapiens (human)
extracellular regionCathepsin D Bos taurus (cattle)
lysosomeCathepsin D Bos taurus (cattle)
melanosomeCathepsin D Bos taurus (cattle)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (7)

Assay IDTitleYearJournalArticle
AID198663Inhibition of human renin at pH 7.01988Journal of medicinal chemistry, Mar, Volume: 31, Issue:3
Inhibition of porcine pepsin by two substrate analogues containing statine. The effect of histidine at the P2 subsite on the inhibition of aspartic proteinases.
AID198512In vitro inhibitory activity against human plasma renin1988Journal of medicinal chemistry, Jan, Volume: 31, Issue:1
Design, structure-activity, and molecular modeling studies of potent renin inhibitory peptides having N-terminal Nin-For-Trp (Ftr): angiotensinogen congeners modified by P1-P1' Phe-Phe, Sta, Leu psi[CH(OH)CH2]Val or leu psi[CH2NH]Val substitutions.
AID198501In vitro inhibition of purified Human kidney renin (250 pg/mL) incubated with angiotensinogen at pH 7.21988Journal of medicinal chemistry, Sep, Volume: 31, Issue:9
Synthesis and biological activity of some transition-state inhibitors of human renin.
AID47834Inhibition of bovine cathepsin D at pH 3.3(no inhibition)1988Journal of medicinal chemistry, Mar, Volume: 31, Issue:3
Inhibition of porcine pepsin by two substrate analogues containing statine. The effect of histidine at the P2 subsite on the inhibition of aspartic proteinases.
AID198981Dissociation constant (Kd) of renin inhibitor was determined over a temperature range of 8-37 degree by the fluorescence displacement assay1990Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
Thermodynamics of the interaction of inhibitors with the binding site of recombinant human renin.
AID198497Inhibition of Human plasma renin1988Journal of medicinal chemistry, Mar, Volume: 31, Issue:3
Renin inhibitors containing psi[CH2O] pseudopeptide inserts.
AID67341Binding affinity against Endothiapepsin2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
SMall Molecule Growth 2001 (SMoG2001): an improved knowledge-based scoring function for protein-ligand interactions.
[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-199013 (72.22)18.7374
1990's4 (22.22)18.2507
2000's1 (5.56)29.6817
2010's0 (0.00)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: 22.53

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 Index22.53 (24.57)
Research Supply Index3.14 (2.92)
Research Growth Index4.02 (4.65)
Search Engine Demand Index23.28 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (22.53)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials2 (10.00%)5.53%
Reviews1 (5.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other17 (85.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]