RSM-932A: a choline kinase inhibitor with antimalarial activity; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 11239948 |
| CHEMBL ID | 192986 |
| MeSH ID | M000600523 |
| Synonym |
|---|
| CHEMBL192986 , |
| 1,1'-([1,1'-biphenyl]-4,4'-diylbis(methylene))bis(4-((4-chlorophenyl)(methyl)amino)quinolin-1-ium) bromide |
| 850807-63-5 |
| choline kinase alpha inhibitor tcd-717 |
| KC1UXA6R4Z , |
| quinolinium, 1,1'-(((1,1'-biphenyl)-4,4'-diyl)bis(methylene))bis(4-((4-chlorophenyl)methylamino)-, bromide (1:2) |
| rsm 932a |
| rsm-932a |
| unii-kc1uxa6r4z |
| MS-31628 |
| HY-101144 |
| 1-[[4-[4-[[4-(4-chloro-n-methylanilino)quinolin-1-ium-1-yl]methyl]phenyl]phenyl]methyl]-n-(4-chlorophenyl)-n-methylquinolin-1-ium-4-amine;dibromide |
| CS-0020908 |
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Choline kinase alpha | Homo sapiens (human) | IC50 (µMol) | 1.9600 | 1.9200 | 1.9600 | 2.0000 | AID1498145; AID241044 |
| Choline kinase | Plasmodium falciparum 3D7 | IC50 (µMol) | 1.7500 | 1.7500 | 1.7500 | 1.7500 | AID1498143 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| lipid metabolic process | Choline kinase alpha | Homo sapiens (human) |
| phosphatidylethanolamine biosynthetic process | Choline kinase alpha | Homo sapiens (human) |
| phosphatidylcholine biosynthetic process | Choline kinase alpha | Homo sapiens (human) |
| lipid transport | Choline kinase alpha | Homo sapiens (human) |
| CDP-choline pathway | Choline kinase alpha | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| choline kinase activity | Choline kinase alpha | Homo sapiens (human) |
| cholinesterase activity | Choline kinase alpha | Homo sapiens (human) |
| ethanolamine kinase activity | Choline kinase alpha | Homo sapiens (human) |
| protein tyrosine kinase activity | Choline kinase alpha | Homo sapiens (human) |
| ATP binding | Choline kinase alpha | Homo sapiens (human) |
| protein homodimerization activity | Choline kinase alpha | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| cytosol | Choline kinase alpha | Homo sapiens (human) |
| lipid droplet | Choline kinase alpha | Homo sapiens (human) |
| cytosol | Choline kinase alpha | Homo sapiens (human) |
| cytoplasm | Choline kinase alpha | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1276679 | Cytotoxicity against human MDA-MB-468 cells after 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2 | Novel Small Molecule Inhibitors of Choline Kinase Identified by Fragment-Based Drug Discovery. |
| AID1498144 | Antiplasmodial activity against Plasmodium falciparum Dd2 infected in human erythrocytes after 48 hrs by picogreen-microfluorimetric assay | 2018 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14 | 1,2-Diphenoxiethane salts as potent antiplasmodial agents. |
| AID1498143 | Inhibition of Plasmodium falciparum 3D7 choline kinase expressed in Escherichia coli BL21(DE3) assessed as reduction in phosphocholine formation | 2018 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14 | 1,2-Diphenoxiethane salts as potent antiplasmodial agents. |
| AID1498145 | Inhibition of human choline kinase alpha1 using [methyl-14C]choline as substrate assessed as reduction in rate of incorporation of 14C from [methyl-14C]choline into phosphocholine preincubated for 5 mins followed by substrate addition measured after 10 mi | 2018 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14 | 1,2-Diphenoxiethane salts as potent antiplasmodial agents. |
| AID1276680 | Cytotoxicity against human MCF10A cells after 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2 | Novel Small Molecule Inhibitors of Choline Kinase Identified by Fragment-Based Drug Discovery. |
| AID247817 | In vitro antiproliferative effect in ras-transformed HT 29 cells | 2005 | Journal of medicinal chemistry, May-05, Volume: 48, Issue:9 | Symmetrical bis-quinolinium compounds: new human choline kinase inhibitors with antiproliferative activity against the HT-29 cell line. |
| AID1498147 | Inhibition of Plasmodium falciparum choline kinase using [methyl-14C]choline as substrate assessed as reduction in rate of incorporation of 14C from [methyl-14C]choline into phosphocholine preincubated for 5 mins followed by substrate addition measured af | 2018 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14 | 1,2-Diphenoxiethane salts as potent antiplasmodial agents. |
| AID241044 | Ex vivo inhibitory concentration against human choline kinase | 2005 | Journal of medicinal chemistry, May-05, Volume: 48, Issue:9 | Symmetrical bis-quinolinium compounds: new human choline kinase inhibitors with antiproliferative activity against the HT-29 cell line. |
| AID1498146 | Antiplasmodial activity against Plasmodium falciparum 3D7 infected in human erythrocytes after 72 hrs by SYBR green 1-based fluorimetric assay | 2018 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14 | 1,2-Diphenoxiethane salts as potent antiplasmodial agents. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 1 (16.67) | 29.6817 |
| 2010's | 4 (66.67) | 24.3611 |
| 2020's | 1 (16.67) | 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 (13.26) 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 | 6 (100.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||