Page last updated: 2024-11-12
leucettamine b
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Description
leucettamine B: a protein kinase inhibitor isolated from the marine sponge Leucetta microraphis; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
Cross-References
| ID Source | ID |
|---|---|
| PubMed CID | 10037501 |
| CHEMBL ID | 485053 |
| SCHEMBL ID | 13219029 |
| MeSH ID | M000611893 |
Synonyms (8)
| Synonym |
|---|
| bdbm50292406 |
| CHEMBL485053 , |
| leucettamine b |
| SCHEMBL13219029 |
| (5z)-2-amino-5-(1,3-benzodioxol-5-ylmethylidene)-3-methylimidazol-4-one |
| STARBLD0021546 |
| 147395-96-8 |
| (z)-2-amino-5-(benzo[d][1,3]dioxol-5-ylmethylene)-3-methyl-3,5-dihydro-4h-imidazol-4-one |
Research Excerpts
Overview
Leucettamine B is a natural product found in marine sponge Leucetta microraphis.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Leucettamine B is a natural product found in marine sponge Leucetta microraphis. " | ( Leucettamine B analogs and their carborane derivative as potential anti-cancer agents: Design, synthesis, and biological evaluation. Chang, JH; Cheng, TM; Chu, HL; Horng, JC; Hsieh, CY; Hsu, KC; Hsu, MH; Kapoor, M; Lin, TE; Tsai, FY, 2020) | 3.44 |
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
Protein Targets (30)
Inhibition Measurements
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Glycogen synthase kinase-3 beta | Sus scrofa (pig) | IC50 (µMol) | 5.9667 | 0.0050 | 1.8419 | 10.0000 | AID1871873; AID606280; AID707501 |
| [Tau protein] kinase | Sus scrofa (pig) | IC50 (µMol) | 5.9667 | 0.0050 | 1.9832 | 10.0000 | AID1871873; AID606280; AID707501 |
| Dual specificity protein kinase CLK2 | Mus musculus (house mouse) | IC50 (µMol) | 1.5200 | 0.1300 | 0.5800 | 2.1000 | AID1871881; AID707688 |
| Dual specificity protein kinase CLK3 | Mus musculus (house mouse) | IC50 (µMol) | 4.7333 | 1.2000 | 3.6800 | 6.4000 | AID1871878; AID606278; AID707687 |
| Dual specificity protein kinase CLK4 | Mus musculus (house mouse) | IC50 (µMol) | 0.1350 | 0.0150 | 0.0944 | 0.6200 | AID1871875; AID707686 |
| Dual specificity tyrosine-phosphorylation-regulated kinase 3 | Homo sapiens (human) | IC50 (µMol) | 1.3500 | 0.0114 | 0.7859 | 3.2000 | AID1871889; AID707506 |
| Cyclin-T1 | Homo sapiens (human) | IC50 (µMol) | 10.0000 | 0.0010 | 0.5585 | 8.0000 | AID707692 |
| Serine/threonine-protein kinase pim-1 | Homo sapiens (human) | IC50 (µMol) | 10.0000 | 0.0004 | 0.8871 | 10.0000 | AID1871892; AID606282; AID707500 |
| Cyclin-A2 | Homo sapiens (human) | IC50 (µMol) | 10.0000 | 0.0004 | 1.0339 | 10.0000 | AID707695 |
| Cannabinoid receptor 1 | Homo sapiens (human) | IC50 (µMol) | 10.0000 | 0.0001 | 0.2753 | 10.0000 | AID1871902 |
| Dual specificity protein kinase CLK1 | Mus musculus (house mouse) | IC50 (µMol) | 0.2020 | 0.0080 | 0.5127 | 4.3000 | AID1871879; AID606277; AID707702 |
| Cyclin-dependent kinase 2 | Homo sapiens (human) | IC50 (µMol) | 10.0000 | 0.0004 | 1.0444 | 10.0000 | AID707695 |
| Kappa-type opioid receptor | Cavia porcellus (domestic guinea pig) | IC50 (µMol) | 5.0330 | 0.0003 | 0.7123 | 7.0700 | AID707693; AID707702 |
| Casein kinase I isoform alpha | Homo sapiens (human) | IC50 (µMol) | 100.0000 | 0.0010 | 2.2499 | 10.0000 | AID470787 |
| Glycogen synthase kinase-3 alpha | Homo sapiens (human) | IC50 (µMol) | 11.3500 | 0.0010 | 1.2249 | 9.1000 | AID470789; AID707503 |
| Glycogen synthase kinase-3 beta | Homo sapiens (human) | IC50 (µMol) | 12.5000 | 0.0006 | 0.8013 | 10.0000 | AID470789; AID707502 |
| Cyclin-dependent kinase 7 | Homo sapiens (human) | IC50 (µMol) | 10.0000 | 0.0001 | 0.9106 | 9.2000 | AID707693 |
| Cyclin-dependent kinase 9 | Homo sapiens (human) | IC50 (µMol) | 10.0000 | 0.0010 | 0.6236 | 8.0000 | AID707692 |
| Cyclin-H | Homo sapiens (human) | IC50 (µMol) | 10.0000 | 0.0005 | 1.0823 | 9.2000 | AID707693 |
| Mitogen-activated protein kinase 1 | Rattus norvegicus (Norway rat) | IC50 (µMol) | 10.0000 | 0.0020 | 0.0818 | 0.2200 | AID707504 |
| Casein kinase II subunit beta | Homo sapiens (human) | IC50 (µMol) | 100.0000 | 0.0003 | 1.4875 | 10.0000 | AID470787 |
| Cyclin-A1 | Homo sapiens (human) | IC50 (µMol) | 10.0000 | 0.0005 | 1.4715 | 10.0000 | AID707695 |
| Cyclin-dependent-like kinase 5 | Homo sapiens (human) | IC50 (µMol) | 40.0000 | 0.0002 | 1.1832 | 10.0000 | AID470788; AID606279; AID707694 |
| Dual specificity tyrosine-phosphorylation-regulated kinase 1A | Homo sapiens (human) | IC50 (µMol) | 0.5900 | 0.0031 | 0.7140 | 9.0120 | AID1871883; AID707509; AID707683 |
| Cyclin-dependent kinase 5 activator 1 | Homo sapiens (human) | IC50 (µMol) | 40.0000 | 0.0010 | 1.2898 | 10.0000 | AID470788; AID606279; AID707694 |
| Leukotriene B4 receptor 1 | Homo sapiens (human) | Ki | 100.0000 | 0.0001 | 0.5126 | 7.0000 | AID337561 |
| Dual specificity tyrosine-phosphorylation-regulated kinase 1A | Rattus norvegicus (Norway rat) | IC50 (µMol) | 1.5400 | 0.0100 | 0.5741 | 2.8000 | AID606275; AID707684; AID707685 |
| Dual specificity tyrosine-phosphorylation-regulated kinase 2 | Homo sapiens (human) | IC50 (µMol) | 1.3100 | 0.0140 | 0.9744 | 3.0000 | AID1871887; AID606276; AID707507 |
| Dual specificity tyrosine-phosphorylation-regulated kinase 4 | Homo sapiens (human) | IC50 (µMol) | 10.0000 | 0.5200 | 4.8000 | 9.5000 | AID707505 |
| Dual specificity tyrosine-phosphorylation-regulated kinase 1B | Homo sapiens (human) | IC50 (µMol) | 2.8500 | 0.0010 | 0.5851 | 4.4200 | AID1871885; AID707508 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Biological Processes (323)
Molecular Functions (71)
Ceullar Components (87)
Bioassays (63)
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID707482 | Binding affinity to CLK1 | 2012 | Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21 | Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B. |
| AID1871895 | Inhibition of human recombinant CK2 at 10 uM using RRRDDDSDDD peptide as substrate incubated for 30 mins in presence of ATP by scintillation counting method | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Structure-Activity Relationship in the Leucettine Family of Kinase Inhibitors. |
| AID707477 | Binding affinity to CLK2 | 2012 | Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21 | Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B. |
| AID1871875 | Inhibition of GST-fused mouse recombinant CLK4 expressed in Escherichia coli using GRSRSRSRSRSR peptide as substrate incubated for 30 mins in presence of ATP by scintillation counting method | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Structure-Activity Relationship in the Leucettine Family of Kinase Inhibitors. |
| AID1871918 | Neuroprotective activity against glutamate-induced cell death in mouse HT-22 cells at 20 uM treated for 24 hrs by MTS assay | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Structure-Activity Relationship in the Leucettine Family of Kinase Inhibitors. |
| AID707501 | Inhibition of pig GSK3alpha/beta isolated from brain using YRRAAVPPSPSLSRHSSPHQ-phosphoS-EDEEE as substrate and [gamma33P]ATP after 30 mins by scintillation counting | 2012 | Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21 | Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B. |
| AID1871883 | Inhibition of GST-fused human recombinant DYRK1A expressed in Escherichia coli using GRSRSRSRSRSR peptide as substrate incubated for 30 mins in presence of ATP by scintillation counting method | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Structure-Activity Relationship in the Leucettine Family of Kinase Inhibitors. |
| AID1871901 | Antagonist activity at CP-55940-activated CB1 receptor (unknown origin) at 10 uM by beta-arrestin assay relative to control | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Structure-Activity Relationship in the Leucettine Family of Kinase Inhibitors. |
| AID606277 | Inhibition of mouse recombinant GST-tagged CLK1 using GRSRSRSRSRSR as substrate | 2011 | Journal of medicinal chemistry, Jun-23, Volume: 54, Issue:12 | Leucettines, a class of potent inhibitors of cdc2-like kinases and dual specificity, tyrosine phosphorylation regulated kinases derived from the marine sponge leucettamine B: modulation of alternative pre-RNA splicing. |
| AID1871900 | Inhibition of DYRK1A in human SH-SY5Y overexpressing Tau4R cells assessed as phosphorylated Tau Thr212 residue level at 10 uM incubated for 6 hrs by western blot analysis relative to control | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Structure-Activity Relationship in the Leucettine Family of Kinase Inhibitors. |
| AID707257 | Inhibition of Plasmodium falciparum recombinant GSK3 expressed in Escherichia coli using YRRAAVPPSPSLSRHSSPHQ-phosphoS-EDEEE as substrate and [gamma33P]ATP at 10 uM after 30 mins by scintillation counting | 2012 | Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21 | Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B. |
| AID1871889 | Inhibition of GST-fused human recombinant DYRK3 expressed in Escherichia coli using GRSRSRSRSRSR peptide as substrate incubated for 30 mins in presence of ATP by scintillation counting method | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Structure-Activity Relationship in the Leucettine Family of Kinase Inhibitors. |
| AID1871916 | Neurotoxicity against mouse HT-22 cells assessed as cell survival at 20 uM treated for 24 hrs by MTS assay | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Structure-Activity Relationship in the Leucettine Family of Kinase Inhibitors. |
| AID707686 | Inhibition of mouse recombinant GST-tagged CLK4 expressed in Escherichia coli using GRSRSRSRSRSR as substrate and [gamma33P]ATP after 30 mins by scintillation counting | 2012 | Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21 | Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B. |
| AID606281 | Inhibition of pig brain CK1 delta/epsilon using RRKHAAIGpSAYSITA as substrate | 2011 | Journal of medicinal chemistry, Jun-23, Volume: 54, Issue:12 | Leucettines, a class of potent inhibitors of cdc2-like kinases and dual specificity, tyrosine phosphorylation regulated kinases derived from the marine sponge leucettamine B: modulation of alternative pre-RNA splicing. |
| AID707683 | Inhibition of human recombinant full length GST-tagged DYRK1A expressed in Escherichia coli using GRSRSRSRSRSR as substrate and [gamma33P]ATP after 30 mins by scintillation counting | 2012 | Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21 | Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B. |
| AID707688 | Inhibition of mouse recombinant GST-tagged CLK2 expressed in Escherichia coli using GRSRSRSRSRSR as substrate and [gamma33P]ATP after 30 mins by scintillation counting | 2012 | Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21 | Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B. |
| AID1871879 | Inhibition of GST-fused mouse recombinant CLK1 expressed in Escherichia coli using GRSRSRSRSRSR peptide as substrate incubated for 30 mins in presence of ATP by scintillation counting method | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Structure-Activity Relationship in the Leucettine Family of Kinase Inhibitors. |
| AID707694 | Inhibition of human recombinant CDK5/p25 using histone H1 as substrate and [gamma33P]ATP after 30 mins by scintillation counting | 2012 | Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21 | Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B. |
| AID707508 | Inhibition of human recombinant GST-tagged DYRK1B expressed in Escherichia coli using GRSRSRSRSRSR as substrate and [gamma33P]ATP after 30 mins by scintillation counting | 2012 | Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21 | Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B. |
| AID606275 | Inhibition of rat recombinant GST-tagged DYRK1A using KKISGRLSPIMTEQ as substrate and [gamma32]-ATP after 30 mins by scintillation counting | 2011 | Journal of medicinal chemistry, Jun-23, Volume: 54, Issue:12 | Leucettines, a class of potent inhibitors of cdc2-like kinases and dual specificity, tyrosine phosphorylation regulated kinases derived from the marine sponge leucettamine B: modulation of alternative pre-RNA splicing. |
| AID707692 | Inhibition of human recombinant CDK9/cyclin T expressed in insect cell using YSPTSPSYSPTSPSYSPTSPSKKKK as substrate and [gamma33P]ATP after 30 mins by scintillation counting | 2012 | Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21 | Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B. |
| AID1871881 | Inhibition of mouse recombinant GST-fused CLK2 expressed in Escherichia coli using GRSRSRSRSRSR peptide as substrate incubated for 30 mins in presence of ATP by scintillation counting method | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Structure-Activity Relationship in the Leucettine Family of Kinase Inhibitors. |
| AID470788 | Inhibition of human CDK5/p25 | 2010 | European journal of medicinal chemistry, Feb, Volume: 45, Issue:2 | Synthesis and preliminary biological evaluation of new derivatives of the marine alkaloid leucettamine B as kinase inhibitors. |
| AID707256 | Inhibition of Leishmania major recombinant CK1 expressed in Escherichia coli using RRKHAAIGpSAYSITA as substrate and [gamma33P]ATP at 10 uM after 30 mins by scintillation counting | 2012 | Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21 | Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B. |
| AID707684 | Inhibition of rat DYRK1A isolated from brain using KKISGRLSPIMTEQ as substrate and [gamma33P]ATP after 30 mins by scintillation counting | 2012 | Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21 | Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B. |
| AID707693 | Inhibition of human recombinant CDK7/cyclin H expressed in insect cell using YSPTSPSYSPTSPSYSPTSPSKKKK as substrate and [gamma33P]ATP after 30 mins by scintillation counting | 2012 | Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21 | Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B. |
| AID707503 | Inhibition of human recombinant GSK3alpha expressed in insect cells using YRRAAVPPSPSLSRHSSPHQ-phosphoS-EDEEE as substrate and [gamma33P]ATP after 30 mins by scintillation counting | 2012 | Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21 | Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B. |
| AID707500 | Inhibition of human recombinant PIM1 expressed in Escherichia coli using histone H1 as substrate and [gamma33P]ATP after 30 mins by scintillation counting | 2012 | Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21 | Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B. |
| AID707480 | Binding affinity to CLK3 | 2012 | Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21 | Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B. |
| AID606280 | Inhibition of pig brain GSK-3alpha/beta using YRRAAVPPSPSLSRHSSPHQSpEDEEE as substrate | 2011 | Journal of medicinal chemistry, Jun-23, Volume: 54, Issue:12 | Leucettines, a class of potent inhibitors of cdc2-like kinases and dual specificity, tyrosine phosphorylation regulated kinases derived from the marine sponge leucettamine B: modulation of alternative pre-RNA splicing. |
| AID707476 | Binding affinity to DYRK1B | 2012 | Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21 | Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B. |
| AID606278 | Inhibition of mouse recombinant GST-tagged CLK3 using GRSRSRSRSRSR as substrate | 2011 | Journal of medicinal chemistry, Jun-23, Volume: 54, Issue:12 | Leucettines, a class of potent inhibitors of cdc2-like kinases and dual specificity, tyrosine phosphorylation regulated kinases derived from the marine sponge leucettamine B: modulation of alternative pre-RNA splicing. |
| AID1871887 | Inhibition of GST-fused human recombinant DYRK2 expressed in Escherichia coli using GRSRSRSRSRSR peptide as substrate incubated for 30 mins in presence of ATP by scintillation counting method | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Structure-Activity Relationship in the Leucettine Family of Kinase Inhibitors. |
| AID606282 | Inhibition of human recombinant Pim1 | 2011 | Journal of medicinal chemistry, Jun-23, Volume: 54, Issue:12 | Leucettines, a class of potent inhibitors of cdc2-like kinases and dual specificity, tyrosine phosphorylation regulated kinases derived from the marine sponge leucettamine B: modulation of alternative pre-RNA splicing. |
| AID707689 | Inhibition of human recombinant CK2 using RRREDEESDDEE as substrate and [gamma33P]ATP at 10 uM after 30 mins by scintillation counting | 2012 | Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21 | Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B. |
| AID707504 | Inhibition of rat recombinant ERK2 using Ets1 as substrate and [gamma33P]ATP as substrate after 30 mins by scintillation counting | 2012 | Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21 | Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B. |
| AID707507 | Inhibition of human recombinant GST-tagged DYRK2 expressed in Escherichia coli using GRSRSRSRSRSR as substrate and [gamma33P]ATP after 30 mins by scintillation counting | 2012 | Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21 | Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B. |
| AID707702 | Inhibition of mouse recombinant GST-tagged CLK1 expressed in Escherichia coli using GRSRSRSRSRSR as substrate and [gamma33P]ATP after 30 mins by scintillation counting | 2012 | Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21 | Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B. |
| AID707696 | Inhibition of starfish CDK1/cyclin B using histone H1 as substrate and [gamma33P]ATP after 30 mins by scintillation counting | 2012 | Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21 | Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B. |
| AID1871873 | Inhibition of porcine brain GSK-3alpha/beta using YRRAAVPPSPSLSRHSSPHQpSEDEEE as substrate incubated for 30 mins in presence of ATP by scintillation counting method | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Structure-Activity Relationship in the Leucettine Family of Kinase Inhibitors. |
| AID337561 | Displacement of [3H]LTB4 from LTB4 receptor expressed in human U937 cell membrane | 1993 | Journal of natural products, Jan, Volume: 56, Issue:1 | New leukotriene B4 receptor antagonist: leucettamine A and related imidazole alkaloids from the marine sponge Leucetta microraphis. |
| AID707691 | Inhibition of pig CD1delta/epsilon isolated from brain using RRKHAAIGpSAYSITA as substrate and [gamma33P]ATP after 30 mins by scintillation couting | 2012 | Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21 | Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B. |
| AID707483 | Binding affinity to DYRK2 | 2012 | Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21 | Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B. |
| AID1871892 | Inhibition of human recombinant Pim1 expressed in Escherichia coli using histone H1 as substrate incubated for 30 mins in presence of ATP by scintillation counting method | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Structure-Activity Relationship in the Leucettine Family of Kinase Inhibitors. |
| AID470787 | Inhibition of human CK1-alpha/CK2beta | 2010 | European journal of medicinal chemistry, Feb, Volume: 45, Issue:2 | Synthesis and preliminary biological evaluation of new derivatives of the marine alkaloid leucettamine B as kinase inhibitors. |
| AID707502 | Inhibition of human recombinant GSK3beta expressed in insect cells using YRRAAVPPSPSLSRHSSPHQ-phosphoS-EDEEE as substrate and [gamma33P]ATP after 30 mins by scintillation counting | 2012 | Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21 | Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B. |
| AID606279 | Inhibition of human recombinant CDK5/p25 | 2011 | Journal of medicinal chemistry, Jun-23, Volume: 54, Issue:12 | Leucettines, a class of potent inhibitors of cdc2-like kinases and dual specificity, tyrosine phosphorylation regulated kinases derived from the marine sponge leucettamine B: modulation of alternative pre-RNA splicing. |
| AID707505 | Inhibition of human recombinant GST-tagged DYRK4 expressed in Escherichia coli using GRSRSRSRSRSR as substrate and [gamma33P]ATP after 30 mins by scintillation counting | 2012 | Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21 | Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B. |
| AID1871878 | Inhibition of GST-fused mouse recombinant CLK3 expressed in Escherichia coli using GRSRSRSRSRSR peptide as substrate incubated for 30 mins in presence of ATP by scintillation counting method | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Structure-Activity Relationship in the Leucettine Family of Kinase Inhibitors. |
| AID707509 | Inhibition of human recombinant C-terminal truncated GST-tagged DYRK1A expressed in Escherichia coli using GRSRSRSRSRSR as substrate and [gamma33P]ATP after 30 mins by scintillation counting | 2012 | Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21 | Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B. |
| AID707485 | Binding affinity to CLK4 | 2012 | Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21 | Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B. |
| AID1871898 | Induction of PI3K/mTor-dependent autophagy in human U2OS cells assessed as number of LC3 foci per cell at 10 uM measured after 4 hrs | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Structure-Activity Relationship in the Leucettine Family of Kinase Inhibitors. |
| AID470789 | Inhibition of human GSK3alpha/ GSK3-beta | 2010 | European journal of medicinal chemistry, Feb, Volume: 45, Issue:2 | Synthesis and preliminary biological evaluation of new derivatives of the marine alkaloid leucettamine B as kinase inhibitors. |
| AID707695 | Inhibition of CDK2/cyclin A using [gamma33P]ATP after 30 mins by scintillation counting | 2012 | Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21 | Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B. |
| AID1871885 | Inhibition of GST-fused human recombinant DYRK1B expressed in Escherichia coli using GRSRSRSRSRSR peptide as substrate incubated for 30 mins in presence of ATP by scintillation counting method | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Structure-Activity Relationship in the Leucettine Family of Kinase Inhibitors. |
| AID707687 | Inhibition of mouse recombinant GST-tagged CLK3 expressed in Escherichia coli using GRSRSRSRSRSR as substrate and [gamma33P]ATP after 30 mins by scintillation counting | 2012 | Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21 | Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B. |
| AID1871899 | Modulation of CLK1 pre-mRNA splicing in mouse HT-22 cells assessed as inclusion of CLK1 exon 4 by measuring change in threshold cycle at 10 uM measured after 4 hrs by real time PCR analysis | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Structure-Activity Relationship in the Leucettine Family of Kinase Inhibitors. |
| AID1871902 | Antagonist activity at CP-55940-activated CB1 receptor (unknown origin) by beta-arrestin assay | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Structure-Activity Relationship in the Leucettine Family of Kinase Inhibitors. |
| AID606276 | Inhibition of human recombinant GST-tagged DYRK2 using KKISGRLSPIMTEQ as substrate and [gamma32]-ATP after 30 mins by scintillation counting | 2011 | Journal of medicinal chemistry, Jun-23, Volume: 54, Issue:12 | Leucettines, a class of potent inhibitors of cdc2-like kinases and dual specificity, tyrosine phosphorylation regulated kinases derived from the marine sponge leucettamine B: modulation of alternative pre-RNA splicing. |
| AID707484 | Binding affinity to DYRK1A | 2012 | Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21 | Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B. |
| AID707685 | Inhibition of rat recombinant C-terminal truncated GST-tagged DYRK1A expressed in Escherichia coli using GRSRSRSRSRSR as substrate and [gamma33P]ATP after 30 mins by scintillation counting | 2012 | Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21 | Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B. |
| AID707506 | Inhibition of human recombinant GST-tagged DYRK3 expressed in Escherichia coli using GRSRSRSRSRSR as substrate and [gamma33P]ATP after 30 mins by scintillation counting | 2012 | Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21 | Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
Research
Studies (10)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 1 (10.00) | 18.2507 |
| 2000's | 0 (0.00) | 29.6817 |
| 2010's | 6 (60.00) | 24.3611 |
| 2020's | 3 (30.00) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
Market Indicators
Research Demand Index: 12.98
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 (12.98) All Compounds (24.57) |
Study Types
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 1 (10.00%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 9 (90.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||