| Assay ID | Title | Year | Journal | Article |
|---|
| AID707499 | Inhibition of Plasmodium falciparum recombinant GSK3 expressed in Escherichia coli 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. |
| AID707489 | Inhibition of human recombinant His6-tagged PIM3 expressed in Sf21 cells using RSRHSSYPAGT as substrate at 10 uM after 30 mins | 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. |
| AID1056640 | Inhibition of human recombinant CDK9/cyclin T using YSPTSPSYSPTSPSYSPTSPSKKKK as substrate | 2013 | European journal of medicinal chemistry, Apr, Volume: 62 | Chemical synthesis and biological validation of immobilized protein kinase inhibitory Leucettines. |
| 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. |
| AID1056636 | Inhibition of mouse recombinant CLK3 expressed in Escherichia coli using GRSRSRSRSRSR as substrate | 2013 | European journal of medicinal chemistry, Apr, Volume: 62 | Chemical synthesis and biological validation of immobilized protein kinase inhibitory Leucettines. |
| AID1056631 | Inhibition of human recombinant DYRK3 expressed in Escherichia coli using GRSRSRSRSRSR as substrate | 2013 | European journal of medicinal chemistry, Apr, Volume: 62 | Chemical synthesis and biological validation of immobilized protein kinase inhibitory Leucettines. |
| AID1459436 | Inhibition of recombinant Leishmania donovani DYRK1B expressed in Escherichia coli using woodtide as substrate after 30 mins in presence of [gamma-33P]ATP by liquid scintillation counting | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Exploration of the imidazo[1,2-b]pyridazine scaffold as a protein kinase inhibitor. |
| AID606356 | Inhibition of CLK4-mediated SRp55 protein phosphorylation in TNFalpha-stimulated human HMEC1 cells after 1 hr by Western blot analysis | 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. |
| AID707260 | Toxicity against CD Sprague-Dawley rat brain expressing human APP at 0.03 to 3 uM after 3 hrs by fluorescence microscopic analysis | 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. |
| AID1871910 | Inhibition of DYRK1A (unknown origin) assessed as maximal inhibition of phosphorylation of Tau Thr212 residue by cell-based 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. |
| AID707267 | Inhibition of DYRK1A in mouse HT22 cells at 10 uM after 4 hrs | 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. |
| AID707452 | Binding affinity to GSK3beta2 in mouse brain homogenate by Western blot analysis | 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. |
| AID707461 | Binding affinity to GSK3beta2 in mouse HT22 cell lysate by Western blot analysis | 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. |
| AID707445 | Downregulation of GSK3 expression in mouse HT22 cells after 4 hrs by Western blot analysis | 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. |
| AID1459442 | Inhibition of recombinant Giardia lamblia CLK expressed in Escherichia coli using RS peptide as substrate after 30 mins in presence of [gamma-33P]ATP by liquid scintillation counting | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Exploration of the imidazo[1,2-b]pyridazine scaffold as a protein kinase inhibitor. |
| 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. |
| AID1459437 | Inhibition of recombinant Leishmania donovani DYRK3 expressed in Escherichia coli using woodtide as substrate after 30 mins in presence of [gamma-33P]ATP by liquid scintillation counting | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Exploration of the imidazo[1,2-b]pyridazine scaffold as a protein kinase inhibitor. |
| 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. |
| AID1056634 | Inhibition of human recombinant DYRK1A expressed in Escherichia coli using GRSRSRSRSRSR as substrate | 2013 | European journal of medicinal chemistry, Apr, Volume: 62 | Chemical synthesis and biological validation of immobilized protein kinase inhibitory Leucettines. |
| AID1871905 | Modulation of CLK1 pre-mRNA splicing in mouse HT-22 cells assessed as maximal effect of CLK1 exon 4 inclusion measured after 3 hrs by qPCR analysis | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2
| Structure-Activity Relationship in the Leucettine Family of Kinase Inhibitors. |
| AID1056639 | Inhibition of porcine brain CK1delta/epsilon using RRKHAAIGpSAYSITA as substrate | 2013 | European journal of medicinal chemistry, Apr, Volume: 62 | Chemical synthesis and biological validation of immobilized protein kinase inhibitory Leucettines. |
| AID707463 | Binding affinity to GSK3alpha in mouse HT22 cell lysate by Western blot analysis | 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. |
| 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. |
| 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. |
| AID1871913 | Induction of PI3K/mTor-dependent autophagy in mouse HT-22 cells assessed as number of LC3 foci per cell at 10 uM incubated for 24 hrs using Lamp-1 staining based immunofluorescence microscopy | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2
| Structure-Activity Relationship in the Leucettine Family of Kinase Inhibitors. |
| AID606291 | Inhibition of recombinant DYRK3-mediated SR 9G8 protein phosphorylation at 10 uM after 30 mins by SDS-PAGE followed by autoradiography | 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. |
| AID707471 | Binding affinity to DYRK1A in mouse brain homogenate after 3 hrs by competition affinity chromatographic analysis | 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. |
| AID707464 | Binding affinity to DYRK1A in mouse HT22 cell lysate by Western blot analysis | 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. |
| AID707451 | Binding affinity to CK2 alpha subunit in mouse brain homogenate by Western blot analysis | 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. |
| 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. |
| 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. |
| 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. |
| AID606295 | Inhibition of recombinant CLK4-mediated SR 9G8 protein phosphorylation at 10 uM after 30 mins by SDS-PAGE followed by autoradiography | 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. |
| 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. |
| AID1871896 | Neurotoxicity against mouse HT-22 cells assessed as cell survival 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. |
| 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. |
| AID707263 | Neuroprotective activity against glutamate-induced toxicity in mouse HT22 cells after 24 hrs by MTS assay | 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. |
| AID707492 | Inhibition of human recombinant GST-tagged DYRK3 expressed in Escherichia coli using KKISGRLSPIMTEQ as substrate at 1 uM after 30 mins | 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. |
| AID606293 | Inhibition of recombinant CLK1-mediated SR 9G8 protein phosphorylation at 10 uM after 30 mins by SDS-PAGE followed by autoradiography | 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. |
| 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. |
| 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. |
| 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. |
| AID707449 | Binding affinity to CK2 beta subunit in mouse brain homogenate by Western blot analysis | 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. |
| AID707459 | Binding affinity to CK2 alpha' subunit in mouse HT22 cell lysate by Western blot analysis | 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. |
| AID707496 | Inhibition of human recombinant GST-tagged DYRK1A expressed in Escherichia coli using KKISGRLSPIMTEQ as substrate at 1 uM after 30 mins | 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. |
| AID707497 | Inhibition of human recombinant GST-tagged DYRK1A expressed in Escherichia coli using KKISGRLSPIMTEQ as substrate at 10 uM after 30 mins | 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. |
| AID707690 | Inhibition of human recombinant CK2 using RRREDEESDDEE 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. |
| AID707479 | Binding affinity to IRAK1 | 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. |
| AID707453 | Binding affinity to GSK3beta1 in mouse brain homogenate by Western blot analysis | 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. |
| AID1871909 | Inhibition of DYRK1A in human SH-SY5Y overexpressing Tau4R cells assessed as reduction in phosphorylation of Tau Thr181 residue level at 10 uM incubated for 6 hrs by western blot analysis | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2
| Structure-Activity Relationship in the Leucettine Family of Kinase Inhibitors. |
| AID707455 | Binding affinity to DYRK1A in mouse brain homogenate by Western blot analysis | 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. |
| AID606354 | Inhibition of CLK2-mediated SRp55 protein phosphorylation in TNFalpha-stimulated human HMEC1 cells after 1 hr by Western blot analysis | 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. |
| 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. |
| AID707265 | Inhibition of CLK1-mediated pre-mRNA splicing in mouse HT22 cells assessed as inclusion of exon 4 after 6 hrs by agarose gel electrophoretic analysis | 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. |
| AID1714121 | Inhibition of human DYRK1A using [33P]-ATP incubated for 120 mins | 2016 | Journal of medicinal chemistry, 11-23, Volume: 59, Issue:22
| An Unusual Binding Model of the Methyl 9-Anilinothiazolo[5,4-f] quinazoline-2-carbimidates (EHT 1610 and EHT 5372) Confers High Selectivity for Dual-Specificity Tyrosine Phosphorylation-Regulated Kinases. |
| AID707268 | Inhibition of GSK3-mediated beta casein phosphorylation in mouse HT22 cells at 0.01 to 10 uM after 24 hrs by Western blot analysis in presence of MG132 | 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. |
| AID707488 | Inhibition of human recombinant His6-tagged PIM3 expressed in Sf21 cells using RSRHSSYPAGT as substrate at 1 uM after 30 mins | 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. |
| AID1871897 | Neuroprotective activity against glutamate-induced cell death in mouse HT-22 cells 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. |
| AID707454 | Binding affinity to GSK3alpha in mouse brain homogenate by Western blot analysis | 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. |
| AID1056630 | Inhibition of porcine brain GSK-3alpha/beta using YRRAAVPPSPSLSRHSSPHQSpEDEEE as substrate | 2013 | European journal of medicinal chemistry, Apr, Volume: 62 | Chemical synthesis and biological validation of immobilized protein kinase inhibitory Leucettines. |
| AID707458 | Binding affinity to CK2 beta subunit in mouse HT22 cell lysate by Western blot analysis | 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. |
| AID707460 | Binding affinity to CK2 alpha subunit in mouse HT22 cell lysate by Western blot analysis | 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. |
| 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. |
| AID1459443 | Inhibition of recombinant Toxoplasma Gondii CLK expressed in Escherichia coli using RS peptide as substrate after 30 mins in presence of [gamma-33P]ATP by liquid scintillation counting | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Exploration of the imidazo[1,2-b]pyridazine scaffold as a protein kinase inhibitor. |
| AID1441348 | Inhibition of CLK1 (unknown origin) | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
| Structural Optimization and Pharmacological Evaluation of Inhibitors Targeting Dual-Specificity Tyrosine Phosphorylation-Regulated Kinases (DYRK) and CDC-like kinases (CLK) in Glioblastoma. |
| AID707475 | Binding affinity to TAOK1 | 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. |
| AID1871908 | Inhibition of DYRK1A in human SH-SY5Y overexpressing Tau4R cells assessed as reduction in phosphorylation of Tau Ser262 residue level at 10 uM incubated for 6 hrs by western blot analysis | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2
| Structure-Activity Relationship in the Leucettine Family of Kinase Inhibitors. |
| AID707487 | Inhibition of CK2 at 10 uM after 30 mins | 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. |
| AID707495 | Inhibition of human recombinant GST-tagged DYRK2 expressed in Escherichia coli using KKISGRLSPIMTEQ as substrate at 1 uM after 30 mins | 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. |
| 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. |
| 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. |
| AID1871907 | Inhibition of DYRK1A in human SH-SY5Y overexpressing Tau4R cells assessed as reduction in phosphorylation of Tau Thr231 residue level at 10 uM incubated for 6 hrs by western blot analysis | 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. |
| 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. |
| AID606292 | Inhibition of recombinant DYRK2-mediated SR 9G8 protein phosphorylation at 10 uM after 30 mins by SDS-PAGE followed by autoradiography | 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. |
| AID1871906 | Inhibition of DYRK1A in human SH-SY5Y overexpressing Tau4R cells assessed as reduction in phosphorylation of Tau Ser202/Thr205 residues level at 10 uM incubated for 6 hrs by western blot analysis | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2
| Structure-Activity Relationship in the Leucettine Family of Kinase Inhibitors. |
| 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. |
| AID1056641 | Inhibition of human recombinant CDK5/p25 using [gamma-33P]-ATP after 30 mins by scintillation counting | 2013 | European journal of medicinal chemistry, Apr, Volume: 62 | Chemical synthesis and biological validation of immobilized protein kinase inhibitory Leucettines. |
| AID1871912 | Neuroprotective activity against glutamate-induced cell death in mouse HT-22 cells at 10 uM incubated for 24 hrs by phase contrast microscopy | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2
| Structure-Activity Relationship in the Leucettine Family of Kinase Inhibitors. |
| 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. |
| AID606289 | Inhibition of pig brain CK1 delta/epsilon using RRKHAAIGpSAYSITA as substrate at 10 uM | 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. |
| AID606294 | Inhibition of recombinant CLK2-mediated SR 9G8 protein phosphorylation at 10 uM after 30 mins by SDS-PAGE followed by autoradiography | 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. |
| 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. |
| 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. |
| AID1056638 | Inhibition of mouse recombinant CLK1 expressed in Escherichia coli using GRSRSRSRSRSR as substrate | 2013 | European journal of medicinal chemistry, Apr, Volume: 62 | Chemical synthesis and biological validation of immobilized protein kinase inhibitory Leucettines. |
| AID1459439 | Inhibition of recombinant Trypanosoma brucei CLK1 expressed in Escherichia coli using RS peptide as substrate after 30 mins in presence of [gamma-33P]ATP by liquid scintillation counting | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Exploration of the imidazo[1,2-b]pyridazine scaffold as a protein kinase inhibitor. |
| AID707261 | Inhibition of DYRK1A in CD Sprague-Dawley rat brain assessed as inhibition of human APP-induced neurodegeneration after 3 hrs by fluorescence microscopic analysis | 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. |
| AID606357 | Inhibition of CLK1-mediated SRp75 protein phosphorylation in TNFalpha-stimulated human HMEC1 cells after 1 hr by Western blot analysis | 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. |
| AID1459440 | Inhibition of recombinant Trypanosoma cruzi CLK1 expressed in Escherichia coli using RS peptide as substrate after 30 mins in presence of [gamma-33P]ATP by liquid scintillation counting | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Exploration of the imidazo[1,2-b]pyridazine scaffold as a protein kinase inhibitor. |
| 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. |
| AID606359 | Inhibition of CLK3-mediated SRp75 protein phosphorylation in TNFalpha-stimulated human HMEC1 cells after 1 hr by Western blot analysis | 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. |
| AID707466 | Binding affinity to phosphatidylinositol-3-phosphate 5-kinase type 3 in mouse brain homogenate after 3 hrs by competition affinity chromatographic analysis | 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. |
| AID1441347 | Inhibition of DYRK1A (unknown origin) | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
| Structural Optimization and Pharmacological Evaluation of Inhibitors Targeting Dual-Specificity Tyrosine Phosphorylation-Regulated Kinases (DYRK) and CDC-like kinases (CLK) in Glioblastoma. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID707490 | Inhibition of human recombinant GST-tagged HIPK2 expressed in Escherichia coli at 1 uM after 30 mins | 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. |
| AID1871911 | Reduction in phosphorylated Tau Thr212 residue in wild-type C57BL/6J mouse brain dosed at 20 mg/kg/day, ip for 19 days by western blot analysis | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2
| Structure-Activity Relationship in the Leucettine Family of Kinase Inhibitors. |
| AID707456 | Binding affinity to VAC14 in mouse HT22 cell lysate by Western blot analysis | 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. |
| AID1056637 | Inhibition of mouse recombinant CLK2 expressed in Escherichia coli using GRSRSRSRSRSR as substrate | 2013 | European journal of medicinal chemistry, Apr, Volume: 62 | Chemical synthesis and biological validation of immobilized protein kinase inhibitory Leucettines. |
| 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. |
| AID1056632 | Inhibition of human recombinant DYRK2 expressed in Escherichia coli using GRSRSRSRSRSR as substrate | 2013 | European journal of medicinal chemistry, Apr, Volume: 62 | Chemical synthesis and biological validation of immobilized protein kinase inhibitory Leucettines. |
| AID1056633 | Inhibition of human recombinant DYRK1B expressed in Escherichia coli using GRSRSRSRSRSR as substrate | 2013 | European journal of medicinal chemistry, Apr, Volume: 62 | Chemical synthesis and biological validation of immobilized protein kinase inhibitory Leucettines. |
| AID1714122 | Inhibition of human DYRK1B using [33P]-ATP incubated for 120 mins | 2016 | Journal of medicinal chemistry, 11-23, Volume: 59, Issue:22
| An Unusual Binding Model of the Methyl 9-Anilinothiazolo[5,4-f] quinazoline-2-carbimidates (EHT 1610 and EHT 5372) Confers High Selectivity for Dual-Specificity Tyrosine Phosphorylation-Regulated Kinases. |
| 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. |
| AID707498 | Inhibition of Leishmania major recombinant CK1 expressed in Escherichia coli using RRKHAAIGpSAYSITA 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. |
| AID707491 | Inhibition of human recombinant GST-tagged HIPK2 expressed in Escherichia coli at 10 uM after 30 mins | 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. |
| AID707473 | Binding affinity to casein kinase 2 | 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. |
| AID1871903 | Drug metabolism in human liver microsomes assessed as GSH reduction metabolite at 50 uM incubated for 60 mins in presence of 13C2,15N-GSH by LC-MS/MS analysis | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2
| Structure-Activity Relationship in the Leucettine Family of Kinase Inhibitors. |
| AID606355 | Inhibition of CLK3-mediated SRp55 protein phosphorylation in TNFalpha-stimulated human HMEC1 cells after 1 hr by Western blot analysis | 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. |
| 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. |
| AID707457 | Binding affinity to phosphatidylinositol-3-phosphate 5-kinase type 3 in mouse HT22 cell lysate by Western blot analysis | 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. |
| AID606361 | Inhibition of CLK1 transfected in human HeLa cells assessed as increase in exon inclusion ratio after 24 hrs by RT-PCR analysis | 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. |
| AID1459444 | Inhibition of recombinant Leishmania major DYRK2 expressed in Escherichia coli using woodtide as substrate after 30 mins in presence of [gamma-33P]ATP by liquid scintillation counting | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Exploration of the imidazo[1,2-b]pyridazine scaffold as a protein kinase inhibitor. |
| AID707264 | Inhibition of CLK4-mediated pre-mRNA splicing in mouse HT22 cells assessed as inclusion of exon 4 after 6 hrs by agarose gel electrophoretic analysis | 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. |
| AID707465 | Binding affinity to VAC14 in mouse brain homogenate after 3 hrs by competition affinity chromatographic analysis | 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. |
| AID707262 | Neuroprotective activity against glutamate-induced toxicity in mouse HT22 cells at 10 to 20 uM up to 48 hrs by MTS assay | 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. |
| AID707447 | Binding affinity to VAC14 in mouse brain homogenate by Western blot analysis | 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. |
| AID707493 | Inhibition of human recombinant GST-tagged DYRK3 expressed in Escherichia coli using KKISGRLSPIMTEQ as substrate at 10 uM after 30 mins | 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. |
| AID1871915 | Displacement of [3H]-CP55940 from CB1 receptor (unknown origin) expressed in HEK293 cell membrane assessed as dissociation constant at 10 uM by liquid 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. |
| AID707448 | Binding affinity to phosphatidylinositol-3-phosphate 5-kinase type 3 in mouse brain homogenate by Western blot analysis | 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. |
| AID1056643 | Inhibition of M phase starfish oocytes CDK1/cyclin B using [gamma-33P]-ATP after 30 mins by scintillation counting | 2013 | European journal of medicinal chemistry, Apr, Volume: 62 | Chemical synthesis and biological validation of immobilized protein kinase inhibitory Leucettines. |
| 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. |
| AID1871894 | Inhibition of human recombinant CK2 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. |
| AID707443 | Inhibition of DYRK1A isolated from mouse HT22 cells | 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. |
| AID707446 | Downregulation of DYRK1A expression in mouse HT22 cells after 4 hrs by Western blot analysis | 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. |
| AID707468 | Binding affinity to CSNK2A2 in mouse brain homogenate after 3 hrs by competition affinity chromatographic analysis | 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. |
| AID707444 | Inhibition of GSK3 isolated from mouse HT22 cells | 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. |
| AID1871874 | Positive allosteric modulation of CB1 receptor (unknown origin) expressed in HEK293 cell membrane assessed as inhibition of CP-55940-induced [35S]-GTPgammaS binding at 10 uM in presence of GDP by liquid scintillation counting method | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2
| Structure-Activity Relationship in the Leucettine Family of Kinase Inhibitors. |
| AID606358 | Inhibition of CLK2-mediated SRp75 protein phosphorylation in TNFalpha-stimulated human HMEC1 cells after 1 hr by Western blot analysis | 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. |
| AID707494 | Inhibition of human recombinant GST-tagged DYRK2 expressed in Escherichia coli using KKISGRLSPIMTEQ as substrate at 10 uM after 30 mins | 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. |
| AID707469 | Binding affinity to CSNK2N in mouse brain homogenate after 3 hrs by competition affinity chromatographic analysis | 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. |
| AID1459446 | Inhibition of recombinant Plasmodium falciparum CLK1 expressed in Escherichia coli using RS peptide as substrate after 30 mins in presence of [gamma-33P]ATP by liquid scintillation counting | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Exploration of the imidazo[1,2-b]pyridazine scaffold as a protein kinase inhibitor. |
| 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. |
| 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. |
| 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. |
| AID1056642 | Inhibition of human recombinant CDK2/cyclin A using [gamma-33P]-ATP after 30 mins by scintillation counting | 2013 | European journal of medicinal chemistry, Apr, Volume: 62 | Chemical synthesis and biological validation of immobilized protein kinase inhibitory Leucettines. |
| AID1871914 | Induction of PI3K/mTor-dependent autophagy in mouse HT-22 cells assessed as number of LC3 foci per cell at 10 uM incubated for 24 hrs using Anti-LC3 staining based immunofluorescence microscopy | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2
| Structure-Activity Relationship in the Leucettine Family of Kinase Inhibitors. |
| AID707266 | Inhibition of GSK3 in mouse HT22 cells at 10 uM after 4 hrs | 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. |
| AID606360 | Inhibition of CLK4-mediated SRp75 protein phosphorylation in TNFalpha-stimulated human HMEC1 cells after 1 hr by Western blot analysis | 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. |
| AID707474 | Binding affinity to GSK3A | 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. |
| AID707478 | Binding affinity to HIPK3 | 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. |
| AID707486 | Inhibition of CK2 at 1 uM after 30 mins | 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. |
| 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. |
| AID1871870 | 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 treated for 6 hrs by qPCR analysis (Rvb = 0.39 +/- 0.25) | 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. |
| AID606296 | Inhibition of CLK1-mediated SRp55 protein phosphorylation in TNFalpha-stimulated human HMEC1 cells after 1 hr by Western blot analysis | 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. |
| AID707470 | Binding affinity to CSNK2A1 in mouse brain homogenate after 3 hrs by competition affinity chromatographic analysis | 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. |
| AID707462 | Binding affinity to GSK3beta1 in mouse HT22 cell lysate by Western blot analysis | 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. |
| AID1871872 | Reduction in phosphorylated Tau Thr212 residue in Tg(Dyrk1a) mutant C57BL/6J mouse brain dosed at 20 mg/kg/day, ip for 19 days by western blot analysis | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2
| Structure-Activity Relationship in the Leucettine Family of Kinase Inhibitors. |
| 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. |
| AID707258 | Inhibition of recombinant SLK assessed as residual activity at 10 uM | 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. |
| AID707467 | Binding affinity to GSK3A in mouse brain homogenate after 3 hrs by competition affinity chromatographic analysis | 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. |
| AID707481 | Binding affinity to HIPK1 | 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. |
| AID1871904 | Drug metabolism in human liver microsomes assessed as GSH demethylation metabolite at 50 uM incubated for 60 mins in presence of 13C2,15N-GSH by LC-MS/MS analysis | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2
| Structure-Activity Relationship in the Leucettine Family of Kinase Inhibitors. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID707450 | Binding affinity to CK2 alpha' subunit in mouse brain homogenate by Western blot analysis | 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. |
| AID707472 | Binding affinity to SLK1 in mouse brain homogenate after 3 hrs by competition affinity chromatographic analysis | 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. |
| AID1459441 | Inhibition of recombinant Cryptosporidium parvum CLK1 expressed in Escherichia coli using RS peptide as substrate after 30 mins in presence of [gamma-33P]ATP by liquid scintillation counting | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Exploration of the imidazo[1,2-b]pyridazine scaffold as a protein kinase inhibitor. |
| AID1056635 | Inhibition of mouse recombinant CLK4 expressed in Escherichia coli using GRSRSRSRSRSR as substrate | 2013 | European journal of medicinal chemistry, Apr, Volume: 62 | Chemical synthesis and biological validation of immobilized protein kinase inhibitory Leucettines. |
| AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1345600 | Human dual specificity tyrosine phosphorylation regulated kinase 2 (Dyrk2 subfamily) | 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. |
| AID1345621 | Mouse CDC like kinase 1 (CLK family) | 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. |
| AID1345695 | Rat dual specificity tyrosine phosphorylation regulated kinase 1A (Dyrk1 subfamily) | 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. |
| AID1345696 | Human dual specificity tyrosine phosphorylation regulated kinase 4 (Dyrk1 subfamily) | 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. |
| AID1345626 | Mouse CDC like kinase 3 (CLK family) | 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. |
| AID1345734 | Human Pim-1 proto-oncogene, serine/threonine kinase (PIM family) | 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. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |