Page last updated: 2024-11-07

bila 2157 bs

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

Description

BILA 2157 BS: renin inhibitor; RN given for (1S-(1R*(S*),2S*,3R*))-isomer; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID157824
CHEMBL ID416472
SCHEMBL ID7387906
MeSH IDM0260097

Synonyms (14)

Synonym
bila 2157 bs
(r)-2-(2-amino-thiazol-4-ylmethyl)-n*4*-cyclohexylmethyl-n*1*-((1s,2r,3s)-1-cyclohexylmethyl-2,3-dihydroxy-5-methyl-hexyl)-n*4*-{[methyl-(2-pyridin-2-yl-ethyl)-carbamoyl]-methyl}-succinamide
bdbm50084627
2-(2-amino-thiazol-4-ylmethyl)-n*4*-cyclohexylmethyl-n*1*-(1-cyclohexylmethyl-2,3-dihydroxy-5-methyl-hexyl)-n*4*-{[methyl-(2-pyridin-2-yl-ethyl)-carbamoyl]-methyl}-succinamide(bila 2157 bs)
CHEMBL416472 ,
(2r)-2-[(2-amino-1,3-thiazol-4-yl)methyl]-n-[(2s,3r,4s)-1-cyclohexyl-3,4-dihydroxy-6-methylheptan-2-yl]-n'-(cyclohexylmethyl)-n'-[2-[methyl(2-pyridin-2-ylethyl)amino]-2-oxoethyl]butanediamide
160937-56-4
bila-2157 bs
(1s-(1r*(s*),2s*,3r*))-2-((2-amino-4-thiazolyl)methyl)-n4-(cyclohexylmethyl)-n1-(1-(cyclohexylmethyl)-2,3-dihydroxy-5-methylhexyl)-n4-(2-(methyl(2-(2-pyridinyl)ethyl)amino)-2-oxoethyl)butanediamide
butanediamide, 2-((2-amino-4-thiazolyl)methyl)-n4-(cyclohexylmethyl)-n1-(1-(cyclohexylmethyl)-2,3-dihydroxy-5-methylhexyl)-n4-(2-(methyl(2-(2-pyridinyl)ethyl)amino)-2-oxoethyl)-, (1s-(1r*(s*),2s*,3r*))-
butanediamide, 2-((2-amino-4-thiazolyl)methyl)-n4-(cyclohexylmethyl)-n'-(1-(cyclohexylmethyl)-2,3-dihydroxy-5-methylhexyl)-n4-(2-(methyl(2-(2-pyridinyl)ethyl)amino)-2-oxoethyl)-, (1s-(1r*(s*),2s*,3r*))-
SCHEMBL7387906
DTXSID40167040
bila2157
[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)
Cathepsin DHomo sapiens (human)IC50 (µMol)0.55000.00000.931610.0000AID219361
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (9)

Processvia Protein(s)Taxonomy
autophagosome assemblyCathepsin DHomo sapiens (human)
proteolysisCathepsin DHomo sapiens (human)
antigen processing and presentation of exogenous peptide antigen via MHC class IICathepsin DHomo sapiens (human)
insulin receptor recyclingCathepsin DHomo sapiens (human)
lipoprotein catabolic processCathepsin DHomo sapiens (human)
positive regulation of apoptotic processCathepsin DHomo sapiens (human)
positive regulation of cysteine-type endopeptidase activity involved in apoptotic processCathepsin DHomo sapiens (human)
regulation of establishment of protein localizationCathepsin DHomo sapiens (human)
insulin catabolic processCathepsin DHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (5)

Processvia Protein(s)Taxonomy
cysteine-type endopeptidase activityCathepsin DHomo sapiens (human)
protein bindingCathepsin DHomo sapiens (human)
peptidase activityCathepsin DHomo sapiens (human)
aspartic-type peptidase activityCathepsin DHomo sapiens (human)
aspartic-type endopeptidase activityCathepsin DHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (14)

Processvia Protein(s)Taxonomy
collagen-containing extracellular matrixCathepsin DHomo sapiens (human)
extracellular regionCathepsin DHomo sapiens (human)
extracellular spaceCathepsin DHomo sapiens (human)
lysosomeCathepsin DHomo sapiens (human)
lysosomal membraneCathepsin DHomo sapiens (human)
endosome membraneCathepsin DHomo sapiens (human)
endosome lumenCathepsin DHomo sapiens (human)
specific granule lumenCathepsin DHomo sapiens (human)
melanosomeCathepsin DHomo sapiens (human)
lysosomal lumenCathepsin DHomo sapiens (human)
membrane raftCathepsin DHomo sapiens (human)
collagen-containing extracellular matrixCathepsin DHomo sapiens (human)
extracellular exosomeCathepsin DHomo sapiens (human)
tertiary granule lumenCathepsin DHomo sapiens (human)
ficolin-1-rich granule lumenCathepsin DHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (6)

Assay IDTitleYearJournalArticle
AID25689Half life period of the compound.1995Journal of medicinal chemistry, May-12, Volume: 38, Issue:10
Time-resolved ligand exchange reactions: kinetic models for competitive inhibitors with recombinant human renin.
AID199004Component acylation rate constant by the compound against Renin was determined1995Journal of medicinal chemistry, May-12, Volume: 38, Issue:10
Time-resolved ligand exchange reactions: kinetic models for competitive inhibitors with recombinant human renin.
AID225413Inhibitory concentration against human plasma renin at pH 6.2000Journal of medicinal chemistry, Feb-10, Volume: 43, Issue:3
Protease inhibitors: current status and future prospects.
AID219361Inhibitory concentration against cathepsin D..2000Journal of medicinal chemistry, Feb-10, Volume: 43, Issue:3
Protease inhibitors: current status and future prospects.
AID24851Oral bioavailability against cynomolgus monkeys at the dose of 3 mg/kg.2000Journal of medicinal chemistry, Feb-10, Volume: 43, Issue:3
Protease inhibitors: current status and future prospects.
AID199005Component acylation rate constant by the compound against Renin was determined1995Journal of medicinal chemistry, May-12, Volume: 38, Issue:10
Time-resolved ligand exchange reactions: kinetic models for competitive inhibitors with recombinant human renin.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (5)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's3 (60.00)18.2507
2000's2 (40.00)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: 12.40

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 Index12.40 (24.57)
Research Supply Index1.79 (2.92)
Research Growth Index4.20 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.40)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (20.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other4 (80.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]