paullone: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
paullone : An indolobenzazepine that is 5,6,7,12-tetrahydroindolo[3,2-d][1]benzazepine carrying an oxo substituent at position 6. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]
| ID Source | ID |
|---|---|
| PubMed CID | 369401 |
| CHEMBL ID | 430574 |
| CHEBI ID | 138487 |
| SCHEMBL ID | 3178594 |
| MeSH ID | M0544184 |
| Synonym |
|---|
| chembl430574 , |
| nsc 641166 |
| bdbm7287 |
| paullone |
| 8,18-diazatetracyclo[9.7.0.0;{2,7}.0;{12,17}]octadeca-1(11),2,4,6,12(17),13,15-heptaen-9-one |
| 7,12-dihydroindolo[3,2-d][1]benzazepin-6(5h)-one |
| 7,12-dihydro-5h-indolo[3,2-d][1]benzazepin-6-one |
| NCI60_013826 |
| nsc641166 |
| nsc-641166 |
| CHEBI:138487 |
| 142273-18-5 |
| FT-0673529 |
| SCHEMBL3178594 |
| DTXSID30327277 |
| J-007629 |
| indolo[3,2-d][1]benzazepin-6(5h)-one, 7,12-dihydro- |
Paullones are a class of molecules structurally based on the 7,12-dihydroindolo[3,2-d]benzazepin-6(5H)-one parent scaffold.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Paullones are a class of molecules structurally based on the 7,12-dihydroindolo[3,2-d][1]benzazepin-6(5H)-one parent scaffold. " | ( Paullones as inhibitors of protein kinases. Kunick, C; Tolle, N, 2011) | 3.25 |
| Role | Description |
|---|---|
| EC 2.7.11.22 (cyclin-dependent kinase) inhibitor | An EC 2.7.11.* (protein-serine/threonine kinase) inhibitor that interferes with the action of cyclin-dependent kinase (EC 2.7.11.22). |
| EC 2.7.11.26 (tau-protein kinase) inhibitor | An EC 2.7.11.* (protein-serine/threonine kinase) inhibitor that interferes with the action of tau-protein kinase inhibitor (EC 2.7.11.26). |
| [role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
| Class | Description |
|---|---|
| lactam | Cyclic amides of amino carboxylic acids, having a 1-azacycloalkan-2-one structure, or analogues having unsaturation or heteroatoms replacing one or more carbon atoms of the ring. |
| indolobenzazepine | An organic heterotetracyclic compound that consists of an indole moiety ortho-fused to any benzazepine. |
| [compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Casein kinase I isoform alpha | Sus scrofa (pig) | IC50 (µMol) | 10.0000 | 1.2000 | 1.2000 | 1.2000 | AID599810 |
| Cyclin-T1 | Homo sapiens (human) | IC50 (µMol) | 0.8100 | 0.0010 | 0.5585 | 8.0000 | AID599805 |
| Glycogen synthase kinase 3 | Plasmodium falciparum 3D7 | IC50 (µMol) | 10.0000 | 0.0230 | 0.2053 | 0.5700 | AID599808 |
| G2/mitotic-specific cyclin-B2 | Homo sapiens (human) | IC50 (µMol) | 6.9992 | 0.0025 | 1.8172 | 10.0000 | AID442242; AID55518 |
| Cyclin-dependent kinase 1 | Homo sapiens (human) | IC50 (µMol) | 6.9996 | 0.0004 | 1.3452 | 10.0000 | AID442242; AID53205; AID55518; AID599814 |
| G2/mitotic-specific cyclin-B1 | Homo sapiens (human) | IC50 (µMol) | 6.9995 | 0.0013 | 1.4518 | 10.0000 | AID442242; AID55518; AID599814 |
| G2/mitotic-specific cyclin-B | Marthasterias glacialis (spiny starfish) | IC50 (µMol) | 5.9067 | 0.0040 | 2.1093 | 9.4000 | AID1796011 |
| Alpha-1B adrenergic receptor | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.8100 | 0.0002 | 1.8742 | 10.0000 | AID599805 |
| Glycogen synthase kinase-3 beta | Rattus norvegicus (Norway rat) | IC50 (µMol) | 5.9067 | 0.0040 | 1.5165 | 7.2000 | AID1796011 |
| Cyclin-A2 | Homo sapiens (human) | IC50 (µMol) | 2.7000 | 0.0004 | 1.0339 | 10.0000 | AID599806 |
| Alpha-1D adrenergic receptor | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.8100 | 0.0002 | 1.2704 | 10.0000 | AID599805 |
| Cyclin-dependent kinase 2 | Homo sapiens (human) | IC50 (µMol) | 2.7000 | 0.0004 | 1.0444 | 10.0000 | AID599806 |
| Alpha-1A adrenergic receptor | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.8100 | 0.0000 | 1.8194 | 10.0000 | AID599805 |
| Dual specificity protein kinase CLK1 | Homo sapiens (human) | IC50 (µMol) | 10.0000 | 0.0074 | 0.4344 | 2.1000 | AID599811 |
| Glycogen synthase kinase-3 beta | Homo sapiens (human) | IC50 (µMol) | 0.3359 | 0.0006 | 0.8013 | 10.0000 | AID1266906; AID442241; AID465257; AID73978 |
| Cyclin-dependent kinase 9 | Homo sapiens (human) | IC50 (µMol) | 0.8100 | 0.0010 | 0.6236 | 8.0000 | AID599805 |
| D(2) dopamine receptor | Rattus norvegicus (Norway rat) | IC50 (µMol) | 10.0000 | 0.0001 | 0.5494 | 8.4000 | AID599810 |
| Cyclin-A1 | Homo sapiens (human) | IC50 (µMol) | 2.7000 | 0.0005 | 1.4715 | 10.0000 | AID599806 |
| Cyclin-dependent-like kinase 5 | Homo sapiens (human) | IC50 (µMol) | 6.4025 | 0.0002 | 1.1832 | 10.0000 | AID1796011; AID54191; AID599809 |
| Cyclin-dependent kinase 5 activator 1 | Homo sapiens (human) | IC50 (µMol) | 6.4025 | 0.0010 | 1.2898 | 10.0000 | AID1796011; AID54191; AID599809 |
| Dual specificity tyrosine-phosphorylation-regulated kinase 1A | Rattus norvegicus (Norway rat) | IC50 (µMol) | 10.0000 | 0.0100 | 0.5741 | 2.8000 | AID599812 |
| NAD-dependent protein deacetylase sirtuin-2 | Homo sapiens (human) | IC50 (µMol) | 31.8667 | 0.5000 | 3.8481 | 10.0000 | AID274367; AID274372; AID274373 |
| G2/mitotic-specific cyclin-B3 | Homo sapiens (human) | IC50 (µMol) | 6.9992 | 0.0025 | 1.8172 | 10.0000 | AID442242; AID55518 |
| NAD-dependent protein deacetylase sirtuin-1 | Homo sapiens (human) | IC50 (µMol) | 29.0000 | 0.0060 | 1.6250 | 9.0000 | AID274370; AID274371 |
| Cyclin-dependent kinase 1 | Oryzias latipes (Japanese medaka) | IC50 (µMol) | 5.9067 | 0.0040 | 2.1093 | 9.4000 | AID1796011 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| G2/mitotic-specific cyclin-B2 | Homo sapiens (human) | ID50 | 7.0000 | 0.0200 | 1.9425 | 7.0000 | AID53336 |
| Cyclin-dependent kinase 1 | Homo sapiens (human) | ID50 | 7.0000 | 0.0200 | 1.9425 | 7.0000 | AID53336 |
| G2/mitotic-specific cyclin-B1 | Homo sapiens (human) | ID50 | 7.0000 | 0.0200 | 1.9425 | 7.0000 | AID53336 |
| G2/mitotic-specific cyclin-B3 | Homo sapiens (human) | ID50 | 7.0000 | 0.0200 | 1.9425 | 7.0000 | AID53336 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID226062 | Inhibition of [3H]naxolone binding to opiate receptors in rat brain | 1993 | Journal of medicinal chemistry, Oct-01, Volume: 36, Issue:20 | Chemistry, binding affinities, and behavioral properties of a new class of "antineophobic" mitochondrial DBI receptor complex (mDRC) ligands. |
| AID274374 | Inhibition of SIRT2 in A549 cells assessed as ability to induce hyperacetylation of tubulin by Western blot analysis | 2006 | Journal of medicinal chemistry, Dec-14, Volume: 49, Issue:25 | Adenosine mimetics as inhibitors of NAD+-dependent histone deacetylases, from kinase to sirtuin inhibition. |
| AID274368 | Inhibition of human SIRT1 at 50 uM | 2006 | Journal of medicinal chemistry, Dec-14, Volume: 49, Issue:25 | Adenosine mimetics as inhibitors of NAD+-dependent histone deacetylases, from kinase to sirtuin inhibition. |
| AID49145 | Inhibitory activity, measured by displacement [3H]CP-55940 from cannabinoid receptor (CB1) in rat brain | 1993 | Journal of medicinal chemistry, Oct-01, Volume: 36, Issue:20 | Chemistry, binding affinities, and behavioral properties of a new class of "antineophobic" mitochondrial DBI receptor complex (mDRC) ligands. |
| AID442241 | Inhibition of GSK3-beta expressed in insect Sf9 cells | 2010 | European journal of medicinal chemistry, Jan, Volume: 45, Issue:1 | Development of 5-benzylpaullones and paullone-9-carboxylic acid alkyl esters as selective inhibitors of mitochondrial malate dehydrogenase (mMDH). |
| AID599810 | Inhibition of porcine brain CK1 assessed as incorporation of [gamma-33P]-ATP into RRKHAAIGpSAYSITA substrate after 30 mins by scintillation counting | 2010 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 20, Issue:16 | Concise synthesis and CDK/GSK inhibitory activity of the missing 9-azapaullones. |
| AID226061 | Tested for inhibitory activity by measuring its ability to displace [3H]3-PPP from opiate receptor in rat brain | 1993 | Journal of medicinal chemistry, Oct-01, Volume: 36, Issue:20 | Chemistry, binding affinities, and behavioral properties of a new class of "antineophobic" mitochondrial DBI receptor complex (mDRC) ligands. |
| AID218972 | Inhibitory activity by measuring its ability to displace [3H]clonidine from alpha-adrenergic receptor in rat brain | 1993 | Journal of medicinal chemistry, Oct-01, Volume: 36, Issue:20 | Chemistry, binding affinities, and behavioral properties of a new class of "antineophobic" mitochondrial DBI receptor complex (mDRC) ligands. |
| AID221928 | Inhibitory activity by measuring its ability to displace [3H]-MK-801 from glutamate(NMDA) receptor in rat brain | 1993 | Journal of medicinal chemistry, Oct-01, Volume: 36, Issue:20 | Chemistry, binding affinities, and behavioral properties of a new class of "antineophobic" mitochondrial DBI receptor complex (mDRC) ligands. |
| AID55518 | Inhibitory activity against cyclin dependent kinase 1-cyclinB extracted from M phase starfish (Marthasterias glacialis) oocytes | 2004 | Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1 | Evaluation and comparison of 3D-QSAR CoMSIA models for CDK1, CDK5, and GSK-3 inhibition by paullones. |
| AID53336 | Inhibition of Cyclin-dependent kinase 1-cyclin B | 2000 | Journal of medicinal chemistry, Jan-13, Volume: 43, Issue:1 | Cyclin-dependent kinase inhibitors: useful targets in cell cycle regulation. |
| AID599805 | Inhibition of human recombinant CDK9/cyclin T expressed in insect cells assessed as incorporation of [gamma-33P]-ATP in to pRB fragment (773 to 928) substrate after 30 mins by scintillation counting | 2010 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 20, Issue:16 | Concise synthesis and CDK/GSK inhibitory activity of the missing 9-azapaullones. |
| AID221360 | Binding affinity against mitochondrial DBI complex (peripheral benzodiazepine receptor) using primary cultures of glial cells | 1993 | Journal of medicinal chemistry, Oct-01, Volume: 36, Issue:20 | Chemistry, binding affinities, and behavioral properties of a new class of "antineophobic" mitochondrial DBI receptor complex (mDRC) ligands. |
| AID599812 | Inhibition of rat recombinant GST-fused DYRK1A expressed in Escherichia coli assessed as assessed as incorporation of [gamma-33P]-ATP into myelin basic protein after 30 mins by scintillation counting | 2010 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 20, Issue:16 | Concise synthesis and CDK/GSK inhibitory activity of the missing 9-azapaullones. |
| AID599806 | Inhibition of human recombinant CDK2/cyclin A assessed as incorporation of [gamma-33P]-ATP into histone H1 substrate after 30 mins by scintillation counting | 2010 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 20, Issue:16 | Concise synthesis and CDK/GSK inhibitory activity of the missing 9-azapaullones. |
| AID80849 | The logarithmic molar concentration inhibiting 50% net cell growth was measured on HCT116 (M) colon cancer cell lines. | 1999 | Journal of medicinal chemistry, Jul-29, Volume: 42, Issue:15 | Paullones, a series of cyclin-dependent kinase inhibitors: synthesis, evaluation of CDK1/cyclin B inhibition, and in vitro antitumor activity. |
| AID274370 | Inhibition of human SIRT1 by fluorescent deacetylase assay | 2006 | Journal of medicinal chemistry, Dec-14, Volume: 49, Issue:25 | Adenosine mimetics as inhibitors of NAD+-dependent histone deacetylases, from kinase to sirtuin inhibition. |
| AID274367 | Inhibition of human recombinant SIRT2 | 2006 | Journal of medicinal chemistry, Dec-14, Volume: 49, Issue:25 | Adenosine mimetics as inhibitors of NAD+-dependent histone deacetylases, from kinase to sirtuin inhibition. |
| AID442242 | Inhibition of CDK1/cyclin B expressed in M phase starfish oocyte | 2010 | European journal of medicinal chemistry, Jan, Volume: 45, Issue:1 | Development of 5-benzylpaullones and paullone-9-carboxylic acid alkyl esters as selective inhibitors of mitochondrial malate dehydrogenase (mMDH). |
| AID53205 | In vitro inhibitory activity against cyclin-dependent kinase 1-cyclin B (Cyclin-Dependent Kinase) harvested from starfish oocytes. | 1999 | Journal of medicinal chemistry, Jul-29, Volume: 42, Issue:15 | Paullones, a series of cyclin-dependent kinase inhibitors: synthesis, evaluation of CDK1/cyclin B inhibition, and in vitro antitumor activity. |
| AID274373 | Inhibition of human recombinant SIRT2 by radioactive deacetylase assay | 2006 | Journal of medicinal chemistry, Dec-14, Volume: 49, Issue:25 | Adenosine mimetics as inhibitors of NAD+-dependent histone deacetylases, from kinase to sirtuin inhibition. |
| AID218903 | Inhibitory activity by measuring its ability to displace [3H]spiperone from dopamine or serotonin 5-HT-1 receptors in rat brain | 1993 | Journal of medicinal chemistry, Oct-01, Volume: 36, Issue:20 | Chemistry, binding affinities, and behavioral properties of a new class of "antineophobic" mitochondrial DBI receptor complex (mDRC) ligands. |
| AID599808 | Inhibition of Plasmodium falciparum GSK3 | 2010 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 20, Issue:16 | Concise synthesis and CDK/GSK inhibitory activity of the missing 9-azapaullones. |
| AID71994 | Inhibitory activity at GABA A receptor, measured by the ability to displace [3H]zolpidem from GABA A receptor in rat brain | 1993 | Journal of medicinal chemistry, Oct-01, Volume: 36, Issue:20 | Chemistry, binding affinities, and behavioral properties of a new class of "antineophobic" mitochondrial DBI receptor complex (mDRC) ligands. |
| AID599814 | Inhibition of CDK1/cyclin B | 2010 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 20, Issue:16 | Concise synthesis and CDK/GSK inhibitory activity of the missing 9-azapaullones. |
| AID218540 | Inhibitory activity by measuring its ability to displace [125I]pindolol from beta-adrenergic receptor in rat brain | 1993 | Journal of medicinal chemistry, Oct-01, Volume: 36, Issue:20 | Chemistry, binding affinities, and behavioral properties of a new class of "antineophobic" mitochondrial DBI receptor complex (mDRC) ligands. |
| AID71991 | Inhibitory activity at GABA A receptor, measured by the ability to displace [35S]TBPS from GABA A receptor in rat brain | 1993 | Journal of medicinal chemistry, Oct-01, Volume: 36, Issue:20 | Chemistry, binding affinities, and behavioral properties of a new class of "antineophobic" mitochondrial DBI receptor complex (mDRC) ligands. |
| AID1266906 | Competitive inhibition of glycogen synthase kinase-3 beta (unknown origin) using GS-1 as substrate after 30 mins by scintillation counting analysis in presence of [gamma-32P]-ATP | 2016 | European journal of medicinal chemistry, Jan-01, Volume: 107 | Pivotal role of glycogen synthase kinase-3: A therapeutic target for Alzheimer's disease. |
| AID442240 | Inhibition of mitochondrial malate dehydrogenase assessed as residual enzyme activity at 10 uM by spectrophotometry | 2010 | European journal of medicinal chemistry, Jan, Volume: 45, Issue:1 | Development of 5-benzylpaullones and paullone-9-carboxylic acid alkyl esters as selective inhibitors of mitochondrial malate dehydrogenase (mMDH). |
| AID599807 | Inhibition of M-phase starfish oocytes CDK1/cyclin B assessed as incorporation of [gamma-33P]-ATP into histone H1 substrate after 30 mins by scintillation counting | 2010 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 20, Issue:16 | Concise synthesis and CDK/GSK inhibitory activity of the missing 9-azapaullones. |
| AID219538 | Inhibitory activity by measuring its ability to displace [3H]L-365260 from cholecystokinin receptor in rat brain | 1993 | Journal of medicinal chemistry, Oct-01, Volume: 36, Issue:20 | Chemistry, binding affinities, and behavioral properties of a new class of "antineophobic" mitochondrial DBI receptor complex (mDRC) ligands. |
| AID92137 | Antitumor activity for each out of 60 human tumor cell lines. | 1999 | Journal of medicinal chemistry, Jul-29, Volume: 42, Issue:15 | Paullones, a series of cyclin-dependent kinase inhibitors: synthesis, evaluation of CDK1/cyclin B inhibition, and in vitro antitumor activity. |
| AID221934 | Inhibitory activity by measuring its ability to displace [3H]glycine from glycine receptor in rat brain | 1993 | Journal of medicinal chemistry, Oct-01, Volume: 36, Issue:20 | Chemistry, binding affinities, and behavioral properties of a new class of "antineophobic" mitochondrial DBI receptor complex (mDRC) ligands. |
| AID599813 | Inhibition of porcine brain GSK3 assessed as incorporation of [gamma-33P]-ATP into YRRAAVPPSPSLSRHSSPHQSpEDEEE after 30 mins by scintillation counting | 2010 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 20, Issue:16 | Concise synthesis and CDK/GSK inhibitory activity of the missing 9-azapaullones. |
| AID599809 | Inhibition of human recombinant CDK5/p25 assessed as incorporation of [gamma-33P]-ATP into histone H1 substrate after 30 mins by scintillation counting | 2010 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 20, Issue:16 | Concise synthesis and CDK/GSK inhibitory activity of the missing 9-azapaullones. |
| AID73978 | Inhibitory activity against glycogen synthase kinase-3 beta purified from insect sf9 cells | 2004 | Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1 | Evaluation and comparison of 3D-QSAR CoMSIA models for CDK1, CDK5, and GSK-3 inhibition by paullones. |
| AID274372 | Inhibition of human recombinant SIRT2 by fluorescent deacetylase assay | 2006 | Journal of medicinal chemistry, Dec-14, Volume: 49, Issue:25 | Adenosine mimetics as inhibitors of NAD+-dependent histone deacetylases, from kinase to sirtuin inhibition. |
| AID229005 | Inhibitory activity by measuring its ability to displace [3H]ketanserin from serotonin receptor in rat brain | 1993 | Journal of medicinal chemistry, Oct-01, Volume: 36, Issue:20 | Chemistry, binding affinities, and behavioral properties of a new class of "antineophobic" mitochondrial DBI receptor complex (mDRC) ligands. |
| AID274371 | Inhibition of human SIRT1 by radioactive deacetylase assay | 2006 | Journal of medicinal chemistry, Dec-14, Volume: 49, Issue:25 | Adenosine mimetics as inhibitors of NAD+-dependent histone deacetylases, from kinase to sirtuin inhibition. |
| AID465257 | Inhibition of human recombinant GSK3-beta assessed as [gamma33]ATP transfer to biotinylated CREB-peptide substrate after 1 hr by scintillation counting | 2010 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5 | Discovery of potent and bioavailable GSK-3beta inhibitors. |
| AID71992 | Inhibitory activity at GABA A receptor, measured by the ability to displace [3H]GABA from GABA A receptor in rat brain | 1993 | Journal of medicinal chemistry, Oct-01, Volume: 36, Issue:20 | Chemistry, binding affinities, and behavioral properties of a new class of "antineophobic" mitochondrial DBI receptor complex (mDRC) ligands. |
| AID218971 | Inhibitory activity by measuring its ability to displace [3H]WB-4101 from alpha-adrenergic receptor in rat brain | 1993 | Journal of medicinal chemistry, Oct-01, Volume: 36, Issue:20 | Chemistry, binding affinities, and behavioral properties of a new class of "antineophobic" mitochondrial DBI receptor complex (mDRC) ligands. |
| AID71993 | Inhibitory activity at GABA A receptor, measured by the ability to displace [3H]flumazenil from GABA A receptor in rat brain | 1993 | Journal of medicinal chemistry, Oct-01, Volume: 36, Issue:20 | Chemistry, binding affinities, and behavioral properties of a new class of "antineophobic" mitochondrial DBI receptor complex (mDRC) ligands. |
| AID54191 | Inhibitory activity against cyclin-dependent kinase 5/p25 | 2004 | Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1 | Evaluation and comparison of 3D-QSAR CoMSIA models for CDK1, CDK5, and GSK-3 inhibition by paullones. |
| AID1424451 | Growth inhibition of human MCF7 cells by MTT assay | 2017 | European journal of medicinal chemistry, Dec-15, Volume: 142 | Indole-fused azepines and analogues as anticancer lead molecules: Privileged findings and future directions. |
| AID221929 | Tested for inhibitory activity by measuring its ability to displace [3H]AMPA from glutamate (non-NMDA) receptor in rat brain | 1993 | Journal of medicinal chemistry, Oct-01, Volume: 36, Issue:20 | Chemistry, binding affinities, and behavioral properties of a new class of "antineophobic" mitochondrial DBI receptor complex (mDRC) ligands. |
| AID71403 | Inhibitory activity at GABA B receptor, measured by the ability to displace [3H]baclofen from GABA B receptor in rat brain | 1993 | Journal of medicinal chemistry, Oct-01, Volume: 36, Issue:20 | Chemistry, binding affinities, and behavioral properties of a new class of "antineophobic" mitochondrial DBI receptor complex (mDRC) ligands. |
| AID599811 | Inhibition of CLK1 | 2010 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 20, Issue:16 | Concise synthesis and CDK/GSK inhibitory activity of the missing 9-azapaullones. |
| AID1796011 | Kinase Inhibition Assay from Article 10.1046/j.1432-1327.2000.01673.x: \\Paullones are potent inhibitors of glycogen synthase kinase-3beta and cyclin-dependent kinase 5/p25.\\ | 2000 | European journal of biochemistry, Oct, Volume: 267, Issue:19 | Paullones are potent inhibitors of glycogen synthase kinase-3beta and cyclin-dependent kinase 5/p25. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 2 (8.70) | 18.2507 |
| 2000's | 4 (17.39) | 29.6817 |
| 2010's | 14 (60.87) | 24.3611 |
| 2020's | 3 (13.04) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.
| This Compound (19.23) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 4 (16.67%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 20 (83.33%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||