Page last updated: 2024-12-08
ent-diltiazem
Description
ent-diltiazem : A 5-[2-(dimethylamino)ethyl]-2-(4-methoxyphenyl)-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepin-3-yl acetate in which both stereocentres have R configuration. It is a cGMP-activated K+ channel blocker. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]
Cross-References
Synonyms (27)
| Synonym |
|---|
| BRD-K81029756-001-02-8 |
| l-(cis)-diltiazem |
| gtpl2349 |
| lopac-d-2521 |
| NCGC00015332-01 |
| NCGC00016818-01 |
| cas-33286-22-5 |
| BSPBIO_001357 |
| NCGC00015332-02 |
| NCGC00163133-03 |
| HMS1989D19 |
| 56209-45-1 |
| HMS1791D19 |
| [(2r,3r)-5-(2-dimethylaminoethyl)-2-(4-methoxyphenyl)-4-oxo-2,3-dihydro-1,5-benzothiazepin-3-yl] acetate |
| NCGC00016818-04 |
| SCHEMBL676914 |
| (2r,3r)-5-[2-(dimethylamino)ethyl]-2-(4-methoxyphenyl)-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepin-3-yl acetate |
| CHEBI:82813 , |
| (-)-cis-diltiazem |
| ent-diltiazem |
| l-cis-diltiazem |
| CHEMBL1397935 |
| cis-3-acetoxy-5-[2-(dimethylamino)ethyl]-2,3-dihydro-2-(4-methoxyphenyl)-1,5-benzothiazepin-4(5h)-one |
| Q27079274 |
| cis-(+)-[2-(2-dimethylaminoethyl)-5-(4-methoxyphenyl)-3-oxo-6-thia-2-azabicyclo[5.4.0]undeca-7,9,11-trien-4-yl] ethanoate |
| [(2r,3r)-5-[2-(dimethylamino)ethyl]-2-(4-methoxyphenyl)-4-oxo-2,3-dihydro-1,5-benzothiazepin-3-yl] acetate |
| 5h0 , |
Roles (1)
| Role | Description |
|---|
| potassium channel blocker | An agent that inhibits cell membrane glycoproteins that are selectively permeable to potassium ions. |
| [role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] |
Drug Classes (1)
| Class | Description |
|---|
| 5-[2-(dimethylamino)ethyl]-2-(4-methoxyphenyl)-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepin-3-yl acetate | A lactam that is 2,3-dihydro-1,5-benzothiazepin-4(5H)-one in which positions 2 and 3 are substituted by 4-methoxyphenyl and acetoxy, respectively, while the hydrogen attached to the nitrogen is substituted by a 2-(dimethylamino)ethyl group. |
| [compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] |
Protein Targets (19)
Potency Measurements
Ceullar Components (1)
Bioassays (5)
| Assay ID | Title | Year | Journal | Article |
|---|
| AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | | | |
| AID1346529 | Rat CNGA2 (Cyclic nucleotide-regulated channels) | 1990 | Nature, Sep-13, Volume: 347, Issue:6289
| Primary structure and functional expression of a cyclic nucleotide-activated channel from olfactory neurons. |
| AID1346482 | Human CNGA1 (Cyclic nucleotide-regulated channels) | 1993 | Nature, Apr-22, Volume: 362, Issue:6422
| A new subunit of the cyclic nucleotide-gated cation channel in retinal rods. |
| AID1346506 | Mouse CNGB3 (Cyclic nucleotide-regulated channels) | 2000 | The Journal of neuroscience : the official journal of the Society for Neuroscience, Feb-15, Volume: 20, Issue:4
| Molecular cloning and functional characterization of a new modulatory cyclic nucleotide-gated channel subunit from mouse retina. |
| AID588519 | A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities | 2011 | Antiviral research, Sep, Volume: 91, Issue:3
| High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Research
Studies (5)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 2 (40.00) | 18.2507 |
| 2000's | 1 (20.00) | 29.6817 |
| 2010's | 1 (20.00) | 24.3611 |
| 2020's | 1 (20.00) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Market Indicators
Research Demand Index: 12.53
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 weak demand-to-supply ratio for research on this compound.
| Metric | This Compound (vs All) |
|---|
| Research Demand Index | 12.53 (24.57) | | Research Supply Index | 1.79 (2.92) | | Research Growth Index | 4.32 (4.65) | | Search Engine Demand Index | 0.00 (26.88) | | Search Engine Supply Index | 0.00 (0.95) |
| |
Study Types
| Publication Type | This drug (%) | All Drugs (%) |
|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 0 (0.00%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 5 (100.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |