LY 97119: clofilium analog; blocks heart potassium channels; structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 194450 |
| CHEMBL ID | 3093959 |
| SCHEMBL ID | 11131309 |
| MeSH ID | M0158524 |
| Synonym |
|---|
| ly 97119 |
| chembl3093959 , |
| bdbm50095760 |
| 72456-59-8 |
| benzenebutanamine, 4-chloro-n-ethyl-n-heptyl- |
| n-[4-(4-chlorophenyl)butyl]-n-ethylheptan-1-amine |
| SCHEMBL11131309 |
| DTXSID70993258 |
| AKOS040748828 |
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Potassium voltage-gated channel subfamily H member 2 | Homo sapiens (human) | IC50 (µMol) | 0.0237 | 0.0009 | 1.9014 | 10.0000 | AID1058738; AID1058739 |
| Potassium voltage-gated channel subfamily H member 2 | Homo sapiens (human) | Ki | 0.0196 | 0.0021 | 1.8407 | 10.0000 | AID1058739; AID1234160 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Potassium voltage-gated channel subfamily H member 2 | Homo sapiens (human) | Kd | 0.0160 | 0.0160 | 0.0160 | 0.0160 | AID1234163 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| plasma membrane | Potassium voltage-gated channel subfamily H member 2 | Homo sapiens (human) |
| cell surface | Potassium voltage-gated channel subfamily H member 2 | Homo sapiens (human) |
| perinuclear region of cytoplasm | Potassium voltage-gated channel subfamily H member 2 | Homo sapiens (human) |
| voltage-gated potassium channel complex | Potassium voltage-gated channel subfamily H member 2 | Homo sapiens (human) |
| inward rectifier potassium channel complex | Potassium voltage-gated channel subfamily H member 2 | Homo sapiens (human) |
| plasma membrane | Potassium voltage-gated channel subfamily H member 2 | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1058739 | Displacement of [3H]astemizole from human ERG channel expressed in HEK293 cell membrane after 1 hr by scintillation counting analysis | 2013 | Journal of medicinal chemistry, Dec-12, Volume: 56, Issue:23 | Removal of human ether-à-go-go related gene (hERG) K+ channel affinity through rigidity: a case of clofilium analogues. |
| AID1234161 | Binding affinity to human Kv11.1 expressed in HEK293 cell membranes assessed as association rate constant by [3H]dofetilide competition association assay | 2015 | Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15 | Structure-Affinity Relationships (SARs) and Structure-Kinetics Relationships (SKRs) of Kv11.1 Blockers. |
| AID1234164 | Binding affinity to human Kv11.1 expressed in HEK293 cell membranes assessed as binding residence time by [3H]dofetilide competition association assay | 2015 | Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15 | Structure-Affinity Relationships (SARs) and Structure-Kinetics Relationships (SKRs) of Kv11.1 Blockers. |
| AID1058738 | Inhibition of human ERG channel expressed in HEK293 cells after 15 mins by whole-cell patch clamp technique | 2013 | Journal of medicinal chemistry, Dec-12, Volume: 56, Issue:23 | Removal of human ether-à-go-go related gene (hERG) K+ channel affinity through rigidity: a case of clofilium analogues. |
| AID1234163 | Binding affinity to human Kv11.1 expressed in HEK293 cell membranes assessed as binding affinity constant by [3H]dofetilide competition association assay | 2015 | Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15 | Structure-Affinity Relationships (SARs) and Structure-Kinetics Relationships (SKRs) of Kv11.1 Blockers. |
| AID1234160 | Displacement of [3H]dofetilide from human Kv11.1 expressed in HEK293 cell membranes by competitive radioligand displacement assay | 2015 | Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15 | Structure-Affinity Relationships (SARs) and Structure-Kinetics Relationships (SKRs) of Kv11.1 Blockers. |
| AID1234162 | Binding affinity to human Kv11.1 expressed in HEK293 cell membranes assessed as dissociation rate constant by [3H]dofetilide competition association assay | 2015 | Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15 | Structure-Affinity Relationships (SARs) and Structure-Kinetics Relationships (SKRs) of Kv11.1 Blockers. |
| AID1058736 | Ratio of Ki for human ERG channel expressed in HEK293 cell membrane after 1 hr by scintillation counting analysis to IC50 for human ERG channel expressed in HEK293 cells after 15 mins by whole-cell patch clamp technique | 2013 | Journal of medicinal chemistry, Dec-12, Volume: 56, Issue:23 | Removal of human ether-à-go-go related gene (hERG) K+ channel affinity through rigidity: a case of clofilium analogues. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 1 (20.00) | 18.7374 |
| 1990's | 2 (40.00) | 18.2507 |
| 2000's | 0 (0.00) | 29.6817 |
| 2010's | 2 (40.00) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
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.
| This Compound (12.72) All Compounds (24.57) |
| 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] | ||