Proteins > G2/mitotic-specific cyclin-B1
Page last updated: 2024-08-07 15:59:09
G2/mitotic-specific cyclin-B1
A G2/mitotic-specific cyclin-B1 that is encoded in the genome of human. [PRO:DAN]
Synonyms
Research
Bioassay Publications (115)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 4 (3.48) | 18.2507 |
| 2000's | 55 (47.83) | 29.6817 |
| 2010's | 48 (41.74) | 24.3611 |
| 2020's | 8 (6.96) | 2.80 |
Compounds (101)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| bisindolylmaleimide i | Homo sapiens (human) | IC50 | 10.6500 | 2 | 2 |
| bisindolylmaleimide iv | Homo sapiens (human) | IC50 | 18.0000 | 1 | 1 |
| bohemine | Homo sapiens (human) | IC50 | 1.1000 | 1 | 1 |
| gw8510 | Homo sapiens (human) | IC50 | 0.0490 | 1 | 1 |
| indirubin-3'-monoxime | Homo sapiens (human) | IC50 | 0.0990 | 2 | 2 |
| nsc 664704 | Homo sapiens (human) | IC50 | 0.4000 | 9 | 9 |
| nu2058 | Homo sapiens (human) | IC50 | 14.6000 | 5 | 5 |
| nu2058 | Homo sapiens (human) | Ki | 5.0000 | 1 | 1 |
| nu6102 | Homo sapiens (human) | IC50 | 0.1329 | 5 | 5 |
| o(6)-benzylguanine | Homo sapiens (human) | IC50 | 24.0000 | 2 | 2 |
| olomoucine | Homo sapiens (human) | IC50 | 89.0714 | 12 | 14 |
| pd 153035 | Homo sapiens (human) | IC50 | 40.2872 | 1 | 5 |
| imatinib | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| indazoles | Homo sapiens (human) | IC50 | 185.0000 | 1 | 1 |
| indirubin | Homo sapiens (human) | IC50 | 11.6250 | 4 | 4 |
| indigo | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| 2-phenylindole | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| staurosporine | Homo sapiens (human) | IC50 | 0.0088 | 14 | 14 |
| baicalin | Homo sapiens (human) | IC50 | 14.3600 | 1 | 1 |
| fascaplysine | Homo sapiens (human) | IC50 | 250.0000 | 1 | 1 |
| o(6)-n-butylguanine | Homo sapiens (human) | IC50 | 32.0000 | 2 | 2 |
| birb 796 | Homo sapiens (human) | IC50 | 30.0000 | 1 | 1 |
| cyc 202 | Homo sapiens (human) | IC50 | 81.1493 | 18 | 27 |
| sb 216763 | Homo sapiens (human) | IC50 | 0.5500 | 1 | 1 |
| 2,4-diamino-6-benzyloxy-5-nitrosopyrimidine | Homo sapiens (human) | IC50 | 27.0000 | 1 | 1 |
| paullone | Homo sapiens (human) | IC50 | 6.9995 | 3 | 3 |
| nu 6027 | Homo sapiens (human) | IC50 | 2.9000 | 2 | 2 |
| nu 6027 | Homo sapiens (human) | Ki | 2.5000 | 1 | 1 |
| meridianin g | Homo sapiens (human) | IC50 | 218.3333 | 2 | 6 |
| 5-iodoindirubin-3'-monoxime | Homo sapiens (human) | IC50 | 0.0250 | 1 | 1 |
| 2H-pyrazolo[4,3-b]quinoxalin-3-amine | Homo sapiens (human) | IC50 | 9.7000 | 1 | 1 |
| 7-n-butyl-6-(4'-hydroxyphenyl)-5h-pyrrolo(2,3b)pyrazine | Homo sapiens (human) | IC50 | 0.1500 | 3 | 3 |
| 6-bromoindirubin-3'-oxime | Homo sapiens (human) | IC50 | 0.3075 | 4 | 4 |
| purvalanol b | Homo sapiens (human) | IC50 | 0.0060 | 3 | 3 |
| purvalanol a | Homo sapiens (human) | IC50 | 0.1026 | 6 | 8 |
| 2-methyl-5-(4-methylanilino)-1,3-benzothiazole-4,7-dione | Homo sapiens (human) | IC50 | 20.0000 | 1 | 1 |
| cgp 60474 | Homo sapiens (human) | IC50 | 0.0260 | 1 | 1 |
| cgp 74514a | Homo sapiens (human) | IC50 | 0.1867 | 3 | 3 |
| 1,4-dimethoxy-10H-acridine-9-thione | Homo sapiens (human) | IC50 | 20.0000 | 1 | 1 |
| bms 387032 | Homo sapiens (human) | IC50 | 0.4800 | 6 | 6 |
| 7-butyl-6-(4-methoxyphenyl)-5H-pyrrolo[2,3-b]pyrazine | Homo sapiens (human) | IC50 | 0.7000 | 1 | 1 |
| 4-benzyl-2-methyl-1,2,4-thiadiazolidine-3,5-dione | Homo sapiens (human) | IC50 | 82.0000 | 3 | 5 |
| sb 415286 | Homo sapiens (human) | IC50 | 0.9000 | 1 | 1 |
| alsterpaullone | Homo sapiens (human) | IC50 | 0.0350 | 3 | 3 |
| quercetin | Homo sapiens (human) | IC50 | 38.3333 | 3 | 3 |
| apigenin | Homo sapiens (human) | IC50 | 4.0000 | 1 | 1 |
| luteolin | Homo sapiens (human) | IC50 | 6.2000 | 1 | 1 |
| kaempferol | Homo sapiens (human) | IC50 | 41.0000 | 1 | 1 |
| harmine | Homo sapiens (human) | IC50 | 18.0000 | 1 | 1 |
| genistein | Homo sapiens (human) | IC50 | 370.0000 | 1 | 1 |
| baicalein | Homo sapiens (human) | IC50 | 6.5300 | 1 | 1 |
| chrysin | Homo sapiens (human) | IC50 | 7.1000 | 1 | 1 |
| fisetin | Homo sapiens (human) | IC50 | 0.7900 | 1 | 1 |
| alvocidib | Homo sapiens (human) | IC50 | 0.1464 | 20 | 26 |
| su 9516 | Homo sapiens (human) | IC50 | 0.0950 | 2 | 2 |
| (E)-3-(2-Hydroxyphenyl)-2-propenal | Homo sapiens (human) | IC50 | 130.0000 | 1 | 1 |
| arcyriaflavin a | Homo sapiens (human) | IC50 | 0.8886 | 4 | 8 |
| pd 0183812 | Homo sapiens (human) | IC50 | 16.0764 | 2 | 5 |
| palbociclib | Homo sapiens (human) | IC50 | 26.6266 | 5 | 5 |
| palbociclib | Homo sapiens (human) | Ki | 5.0000 | 1 | 1 |
| jnj-7706621 | Homo sapiens (human) | IC50 | 29.5281 | 2 | 15 |
| olomoucine ii | Homo sapiens (human) | IC50 | 0.0200 | 1 | 1 |
| vx680 | Homo sapiens (human) | IC50 | 0.0092 | 1 | 2 |
| cyc 116 | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| 1-azakenpaullone | Homo sapiens (human) | IC50 | 2.0000 | 3 | 3 |
| 2-[(3-iodophenyl)methylthio]-5-pyridin-4-yl-1,3,4-oxadiazole | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| b 43 | Homo sapiens (human) | IC50 | 50.0000 | 1 | 1 |
| aminopurvalanol a | Homo sapiens (human) | IC50 | 0.0340 | 1 | 2 |
| cvt 313 | Homo sapiens (human) | IC50 | 3.7000 | 1 | 1 |
| npi 2358 | Homo sapiens (human) | IC50 | 10.1000 | 1 | 0 |
| chir 99021 | Homo sapiens (human) | IC50 | 8.8000 | 1 | 1 |
| nu 6140 | Homo sapiens (human) | IC50 | 5.8000 | 1 | 1 |
| meridianin a | Homo sapiens (human) | IC50 | 36.7167 | 2 | 6 |
| rgb 286638 | Homo sapiens (human) | IC50 | 0.0020 | 1 | 1 |
| at 7519 | Homo sapiens (human) | IC50 | 0.1682 | 7 | 8 |
| at 7519 | Homo sapiens (human) | Ki | 0.1900 | 1 | 1 |
| pf 573228 | Homo sapiens (human) | IC50 | 0.7430 | 2 | 2 |
| crizotinib | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| pha 848125 | Homo sapiens (human) | IC50 | 0.4661 | 4 | 8 |
| 14-methyl-20-oxa-5,7,14,26-tetraazatetracyclo(19.3.1.1(2,6).1(8,12))heptacosa-1(25),2(26),3,5,8(27),9,11,16,21,23-decaene | Homo sapiens (human) | IC50 | 0.0090 | 1 | 1 |
| azd5438 | Homo sapiens (human) | IC50 | 0.0160 | 1 | 1 |
| p276-00 | Homo sapiens (human) | IC50 | 0.0790 | 1 | 1 |
| cx 4945 | Homo sapiens (human) | IC50 | 0.0560 | 2 | 2 |
| cink4 | Homo sapiens (human) | IC50 | 54.6000 | 2 | 2 |
| ldc067 | Homo sapiens (human) | IC50 | 3.9500 | 1 | 1 |
| bs 194 | Homo sapiens (human) | IC50 | 0.0330 | 1 | 1 |
| (R)-DRF053 | Homo sapiens (human) | IC50 | 1.9600 | 2 | 2 |
| 4-[6-[4-(methoxycarbonylamino)phenyl]-4-(4-morpholinyl)-1-pyrazolo[3,4-d]pyrimidinyl]-1-piperidinecarboxylic acid methyl ester | Homo sapiens (human) | IC50 | 50.0000 | 1 | 1 |
| ribociclib | Homo sapiens (human) | IC50 | 20.0000 | 2 | 2 |
| bay 1000394 | Homo sapiens (human) | IC50 | 0.0070 | 4 | 4 |
| pha 793887 | Homo sapiens (human) | IC50 | 0.0600 | 1 | 1 |
| tak-632 | Homo sapiens (human) | IC50 | 0.7900 | 1 | 1 |
| abemaciclib | Homo sapiens (human) | IC50 | 0.7484 | 6 | 6 |
| abemaciclib | Homo sapiens (human) | Ki | 1.6270 | 1 | 1 |
| dinaciclib | Homo sapiens (human) | IC50 | 0.0490 | 3 | 3 |
| nms p937 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| gilteritinib | Homo sapiens (human) | Ki | 5.0000 | 1 | 1 |
| bs-181 | Homo sapiens (human) | IC50 | 14.0000 | 1 | 1 |
| butyrolactone i | Homo sapiens (human) | IC50 | 0.6000 | 2 | 2 |
| on123300 | Homo sapiens (human) | IC50 | 0.6000 | 1 | 1 |
| amg 925 | Homo sapiens (human) | IC50 | 2.2200 | 1 | 1 |
| at 9283 | Homo sapiens (human) | IC50 | 1.7000 | 1 | 1 |
| can 508 | Homo sapiens (human) | IC50 | 32.6062 | 3 | 8 |
| ro 3306 | Homo sapiens (human) | IC50 | 0.0470 | 1 | 1 |
| hymenialdisine | Homo sapiens (human) | IC50 | 0.0220 | 3 | 3 |
| debromohymenialdisine | Homo sapiens (human) | IC50 | 8.6661 | 1 | 7 |
Drugs with Other Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| nsc 664704 | Homo sapiens (human) | ID50 | 0.2175 | 2 | 2 |
| olomoucine | Homo sapiens (human) | ID50 | 7.0000 | 1 | 1 |
| cyc 202 | Homo sapiens (human) | ID50 | 0.6500 | 1 | 1 |
| paullone | Homo sapiens (human) | ID50 | 7.0000 | 1 | 1 |
| cgp 60474 | Homo sapiens (human) | ID50 | 0.0200 | 1 | 1 |
| alsterpaullone | Homo sapiens (human) | ID50 | 0.0350 | 1 | 1 |
| alvocidib | Homo sapiens (human) | ID50 | 0.4000 | 1 | 1 |
Indole-fused azepines and analogues as anticancer lead molecules: Privileged findings and future directions.European journal of medicinal chemistry, , Dec-15, Volume: 142, 2017
Discovery of novel CDK1 inhibitors by combining pharmacophore modeling, QSAR analysis and in silico screening followed by in vitro bioassay.European journal of medicinal chemistry, , Volume: 45, Issue:9, 2010
Concise synthesis and CDK/GSK inhibitory activity of the missing 9-azapaullones.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 20, Issue:16, 2010
Development of 5-benzylpaullones and paullone-9-carboxylic acid alkyl esters as selective inhibitors of mitochondrial malate dehydrogenase (mMDH).European journal of medicinal chemistry, , Volume: 45, Issue:1, 2010
1-Azakenpaullone is a selective inhibitor of glycogen synthase kinase-3 beta.Bioorganic & medicinal chemistry letters, , Jan-19, Volume: 14, Issue:2, 2004
Evaluation and comparison of 3D-QSAR CoMSIA models for CDK1, CDK5, and GSK-3 inhibition by paullones.Journal of medicinal chemistry, , Jan-01, Volume: 47, Issue:1, 2004
Pharmacological inhibitors of glycogen synthase kinase 3.Trends in pharmacological sciences, , Volume: 25, Issue:9, 2004
Evaluation of the first cytostatically active 1-aza-9-oxafluorenes as novel selective CDK1 inhibitors with P-glycoprotein modulating properties.Journal of medicinal chemistry, , Feb-27, Volume: 46, Issue:5, 2003
2-Substituted paullones: CDK1/cyclin B-inhibiting property and in vitro antiproliferative activity.Bioorganic & medicinal chemistry letters, , Mar-20, Volume: 10, Issue:6, 2000
Cyclin-dependent kinase inhibitors: useful targets in cell cycle regulation.Journal of medicinal chemistry, , Jan-13, Volume: 43, Issue:1, 2000
Cyclin-Dependent Kinase (CDK) Inhibitors: Structure-Activity Relationships and Insights into the CDK-2 Selectivity of 6-Substituted 2-Arylaminopurines.Journal of medicinal chemistry, , 03-09, Volume: 60, Issue:5, 2017
8-Substituted O(6)-cyclohexylmethylguanine CDK2 inhibitors: using structure-based inhibitor design to optimize an alternative binding mode.Journal of medicinal chemistry, , Jan-09, Volume: 57, Issue:1, 2014
Discovery of kinase inhibitors by high-throughput docking and scoring based on a transferable linear interaction energy model.Journal of medicinal chemistry, , Mar-13, Volume: 51, Issue:5, 2008
N2-substituted O6-cyclohexylmethylguanine derivatives: potent inhibitors of cyclin-dependent kinases 1 and 2.Journal of medicinal chemistry, , Jul-15, Volume: 47, Issue:15, 2004
Probing the ATP ribose-binding domain of cyclin-dependent kinases 1 and 2 with O(6)-substituted guanine derivatives.Journal of medicinal chemistry, , Aug-01, Volume: 45, Issue:16, 2002
How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases?Journal of medicinal chemistry, , 10-25, Volume: 61, Issue:20, 2018
Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase 1A (DYRK1A) Inhibitors as Potential Therapeutics.Journal of medicinal chemistry, , 11-21, Volume: 61, Issue:22, 2018
Cyclin-Dependent Kinase (CDK) Inhibitors: Structure-Activity Relationships and Insights into the CDK-2 Selectivity of 6-Substituted 2-Arylaminopurines.Journal of medicinal chemistry, , 03-09, Volume: 60, Issue:5, 2017
8-Substituted O(6)-cyclohexylmethylguanine CDK2 inhibitors: using structure-based inhibitor design to optimize an alternative binding mode.Journal of medicinal chemistry, , Jan-09, Volume: 57, Issue:1, 2014
N2-substituted O6-cyclohexylmethylguanine derivatives: potent inhibitors of cyclin-dependent kinases 1 and 2.Journal of medicinal chemistry, , Jul-15, Volume: 47, Issue:15, 2004
Discovery of kinase inhibitors by high-throughput docking and scoring based on a transferable linear interaction energy model.Journal of medicinal chemistry, , Mar-13, Volume: 51, Issue:5, 2008
Probing the ATP ribose-binding domain of cyclin-dependent kinases 1 and 2 with O(6)-substituted guanine derivatives.Journal of medicinal chemistry, , Aug-01, Volume: 45, Issue:16, 2002
An appraisal on synthetic and pharmaceutical perspectives of pyrazolo[4,3-d]pyrimidine scaffold.Bioorganic & medicinal chemistry, , 01-15, Volume: 26, Issue:2, 2018
Discovery of novel CDK1 inhibitors by combining pharmacophore modeling, QSAR analysis and in silico screening followed by in vitro bioassay.European journal of medicinal chemistry, , Volume: 45, Issue:9, 2010
Synthesis and cytotoxic activity of 2-methylimidazo[1,2-a]pyridine- and quinoline-substituted 2-aminopyrimidine derivatives.European journal of medicinal chemistry, , Volume: 45, Issue:1, 2010
Pyrrolo[2,3-a]carbazoles as potential cyclin dependent kinase 1 (CDK1) Inhibitors. Synthesis, biological evaluation, and binding mode through docking simulations.Journal of medicinal chemistry, , Feb-28, Volume: 51, Issue:4, 2008
Pyrazolo[4,3-d]pyrimidines as new generation of cyclin-dependent kinase inhibitors.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 13, Issue:18, 2003
Synthesis and biological activity of olomoucine II.Bioorganic & medicinal chemistry letters, , Nov-18, Volume: 12, Issue:22, 2002
Structural classification of protein kinases using 3D molecular interaction field analysis of their ligand binding sites: target family landscapes.Journal of medicinal chemistry, , Jun-06, Volume: 45, Issue:12, 2002
Cyclin-dependent kinase inhibition by new C-2 alkynylated purine derivatives and molecular structure of a CDK2-inhibitor complex.Journal of medicinal chemistry, , Apr-06, Volume: 43, Issue:7, 2000
Thio- and oxoflavopiridols, cyclin-dependent kinase 1-selective inhibitors: synthesis and biological effects.Journal of medicinal chemistry, , Nov-02, Volume: 43, Issue:22, 2000
Cyclin-dependent kinase inhibitors: useful targets in cell cycle regulation.Journal of medicinal chemistry, , Jan-13, Volume: 43, Issue:1, 2000
Synthesis of C2 alkynylated purines, a new family of potent inhibitors of cyclin-dependent kinases.Bioorganic & medicinal chemistry letters, , Apr-07, Volume: 8, Issue:7, 1998
Identification of a Water-Soluble Indirubin Derivative as Potent Inhibitor of Insulin-like Growth Factor 1 Receptor through Structural Modification of the Parent Natural Molecule.Journal of medicinal chemistry, , 06-22, Volume: 60, Issue:12, 2017
Generation of new protein kinase inhibitors utilizing cytochrome p450 mutant enzymes for indigoid synthesis.Journal of medicinal chemistry, , Jun-03, Volume: 47, Issue:12, 2004
Structural basis for the synthesis of indirubins as potent and selective inhibitors of glycogen synthase kinase-3 and cyclin-dependent kinases.Journal of medicinal chemistry, , Feb-12, Volume: 47, Issue:4, 2004
Chemistry-oriented synthesis (ChOS) and target deconvolution on neuroprotective effect of a novel scaffold, oxaza spiroquinone.European journal of medicinal chemistry, , Feb-01, Volume: 163, 2019
ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells.European journal of medicinal chemistry, , Jan-01, Volume: 161, 2019
New insights in the structure-activity relationships of 2-phenylamino-substituted benzothiopyrano[4,3-d]pyrimidines as kinase inhibitors.European journal of medicinal chemistry, , Apr-25, Volume: 150, 2018
Challenging clinically unresponsive medullary thyroid cancer: Discovery and pharmacological activity of novel RET inhibitors.European journal of medicinal chemistry, , Apr-25, Volume: 150, 2018
Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors.Bioorganic & medicinal chemistry, , 05-01, Volume: 26, Issue:8, 2018
Novel LCK/FMS inhibitors based on phenoxypyrimidine scaffold as potential treatment for inflammatory disorders.European journal of medicinal chemistry, , Dec-01, Volume: 141, 2017
Discovery of 4-arylamido 3-methyl isoxazole derivatives as novel FMS kinase inhibitors.European journal of medicinal chemistry, , Sep-18, Volume: 102, 2015
Syntheses of phenylpyrazolodiazepin-7-ones as conformationally rigid analogs of aminopyrazole amide scaffold and their antiproliferative effects on cancer cells.Bioorganic & medicinal chemistry, , Nov-15, Volume: 19, Issue:22, 2011
From a natural product lead to the identification of potent and selective benzofuran-3-yl-(indol-3-yl)maleimides as glycogen synthase kinase 3beta inhibitors that suppress proliferation and survival of pancreatic cancer cells.Journal of medicinal chemistry, , Apr-09, Volume: 52, Issue:7, 2009
Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells.Journal of medicinal chemistry, , May-28, Volume: 52, Issue:10, 2009
Selectivity and potency of cyclin-dependent kinase inhibitors.The AAPS journal, , Mar-24, Volume: 8, Issue:1, 2006
Synthesis and biological evaluation of 1-aryl-4,5-dihydro-1H-pyrazolo[3,4-d]pyrimidin-4-one inhibitors of cyclin-dependent kinases.Journal of medicinal chemistry, , Nov-18, Volume: 47, Issue:24, 2004
Pharmacological inhibitors of glycogen synthase kinase 3.Trends in pharmacological sciences, , Volume: 25, Issue:9, 2004
Aryl[a]pyrrolo[3,4-c]carbazoles as selective cyclin D1-CDK4 inhibitors.Bioorganic & medicinal chemistry letters, , Nov-03, Volume: 13, Issue:21, 2003
Discovery of kinase inhibitors by high-throughput docking and scoring based on a transferable linear interaction energy model.Journal of medicinal chemistry, , Mar-13, Volume: 51, Issue:5, 2008
Probing the ATP ribose-binding domain of cyclin-dependent kinases 1 and 2 with O(6)-substituted guanine derivatives.Journal of medicinal chemistry, , Aug-01, Volume: 45, Issue:16, 2002
Design, synthesis, and biological evaluation of 4-benzoylamino-1H-pyrazole-3-carboxamide derivatives as potent CDK2 inhibitors.European journal of medicinal chemistry, , Apr-05, Volume: 215, 2021
[no title available]Bioorganic & medicinal chemistry, , 09-01, Volume: 28, Issue:17, 2020
Identification of a Water-Soluble Indirubin Derivative as Potent Inhibitor of Insulin-like Growth Factor 1 Receptor through Structural Modification of the Parent Natural Molecule.Journal of medicinal chemistry, , 06-22, Volume: 60, Issue:12, 2017
RETRACTED: Design, synthesis, structure-activity relationship and kinase inhibitory activity of substituted 3-methyl-1-phenyl-1H-pyrazolo[3,4-d]pyrimidin-4-ones.Bioorganic & medicinal chemistry letters, , 07-01, Volume: 26, Issue:13, 2016
Discovery of 8-cyclopentyl-2-[4-(4-methyl-piperazin-1-yl)-phenylamino]-7-oxo-7,8-dihydro-pyrido[2,3-d]pyrimidine-6-carbonitrile (7x) as a potent inhibitor of cyclin-dependent kinase 4 (CDK4) and AMPK-related kinase 5 (ARK5).Journal of medicinal chemistry, , Feb-13, Volume: 57, Issue:3, 2014
Potent inhibitors of CDK5 derived from roscovitine: synthesis, biological evaluation and molecular modelling.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 23, Issue:1, 2013
Synthesis and biological evaluation of guanidino analogues of roscovitine.European journal of medicinal chemistry, , Volume: 62, 2013
Design, synthesis and biological evaluation of 6-pyridylmethylaminopurines as CDK inhibitors.Bioorganic & medicinal chemistry, , Nov-15, Volume: 19, Issue:22, 2011
A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration.Journal of medicinal chemistry, , Dec-23, Volume: 53, Issue:24, 2010
Pyrazolo[1,5-a]-1,3,5-triazine as a purine bioisostere: access to potent cyclin-dependent kinase inhibitor (R)-roscovitine analogue.Journal of medicinal chemistry, , Feb-12, Volume: 52, Issue:3, 2009
Identification of N-(4-piperidinyl)-4-(2,6-dichlorobenzoylamino)-1H-pyrazole-3-carboxamide (AT7519), a novel cyclin dependent kinase inhibitor using fragment-based X-ray crystallography and structure based drug design.Journal of medicinal chemistry, , Aug-28, Volume: 51, Issue:16, 2008
Novel 9-oxo-thiazolo[5,4-f]quinazoline-2-carbonitrile derivatives as dual cyclin-dependent kinase 1 (CDK1)/glycogen synthase kinase-3 (GSK-3) inhibitors: synthesis, biological evaluation and molecular modeling studies.European journal of medicinal chemistry, , Volume: 43, Issue:7, 2008
Meridianins, a new family of protein kinase inhibitors isolated from the ascidian Aplidium meridianum.Bioorganic & medicinal chemistry letters, , Apr-05, Volume: 14, Issue:7, 2004
Synthesis and biological activity of olomoucine II.Bioorganic & medicinal chemistry letters, , Nov-18, Volume: 12, Issue:22, 2002
Structural classification of protein kinases using 3D molecular interaction field analysis of their ligand binding sites: target family landscapes.Journal of medicinal chemistry, , Jun-06, Volume: 45, Issue:12, 2002
Cyclin-dependent kinase inhibition by new C-2 alkynylated purine derivatives and molecular structure of a CDK2-inhibitor complex.Journal of medicinal chemistry, , Apr-06, Volume: 43, Issue:7, 2000
Cyclin-dependent kinase inhibitors: useful targets in cell cycle regulation.Journal of medicinal chemistry, , Jan-13, Volume: 43, Issue:1, 2000
Synthesis of C2 alkynylated purines, a new family of potent inhibitors of cyclin-dependent kinases.Bioorganic & medicinal chemistry letters, , Apr-07, Volume: 8, Issue:7, 1998
Concise synthesis and CDK/GSK inhibitory activity of the missing 9-azapaullones.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 20, Issue:16, 2010
Development of 5-benzylpaullones and paullone-9-carboxylic acid alkyl esters as selective inhibitors of mitochondrial malate dehydrogenase (mMDH).European journal of medicinal chemistry, , Volume: 45, Issue:1, 2010
Evaluation and comparison of 3D-QSAR CoMSIA models for CDK1, CDK5, and GSK-3 inhibition by paullones.Journal of medicinal chemistry, , Jan-01, Volume: 47, Issue:1, 2004
Cyclin-dependent kinase inhibitors: useful targets in cell cycle regulation.Journal of medicinal chemistry, , Jan-13, Volume: 43, Issue:1, 2000
6-Cyclohexylmethoxy-5-(cyano-NNO-azoxy)pyrimidine-4-amine: a new scaffold endowed with potent CDK2 inhibitory activity.European journal of medicinal chemistry, , Volume: 68, 2013
4-Alkoxy-2,6-diaminopyrimidine derivatives: inhibitors of cyclin dependent kinases 1 and 2.Bioorganic & medicinal chemistry letters, , Jan-20, Volume: 13, Issue:2, 2003
Identification of novel purine and pyrimidine cyclin-dependent kinase inhibitors with distinct molecular interactions and tumor cell growth inhibition profiles.Journal of medicinal chemistry, , Jul-27, Volume: 43, Issue:15, 2000
Recent development of CDK inhibitors: An overview of CDK/inhibitor co-crystal structures.European journal of medicinal chemistry, , Feb-15, Volume: 164, 2019
Pharmacological inhibitors of glycogen synthase kinase 3.Trends in pharmacological sciences, , Volume: 25, Issue:9, 2004
Aloisines, a new family of CDK/GSK-3 inhibitors. SAR study, crystal structure in complex with CDK2, enzyme selectivity, and cellular effects.Journal of medicinal chemistry, , Jan-16, Volume: 46, Issue:2, 2003
How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases?Journal of medicinal chemistry, , 10-25, Volume: 61, Issue:20, 2018
Soluble 3',6-substituted indirubins with enhanced selectivity toward glycogen synthase kinase -3 alter circadian period.Journal of medicinal chemistry, , Oct-23, Volume: 51, Issue:20, 2008
Pharmacological inhibitors of glycogen synthase kinase 3.Trends in pharmacological sciences, , Volume: 25, Issue:9, 2004
Structural basis for the synthesis of indirubins as potent and selective inhibitors of glycogen synthase kinase-3 and cyclin-dependent kinases.Journal of medicinal chemistry, , Feb-12, Volume: 47, Issue:4, 2004
Structural classification of protein kinases using 3D molecular interaction field analysis of their ligand binding sites: target family landscapes.Journal of medicinal chemistry, , Jun-06, Volume: 45, Issue:12, 2002
Cyclin-dependent kinase inhibition by new C-2 alkynylated purine derivatives and molecular structure of a CDK2-inhibitor complex.Journal of medicinal chemistry, , Apr-06, Volume: 43, Issue:7, 2000
Exploiting chemical libraries, structure, and genomics in the search for kinase inhibitors.Science (New York, N.Y.), , Jul-24, Volume: 281, Issue:5376, 1998
[1,2]Oxazolo[5,4-e]isoindoles as promising tubulin polymerization inhibitors.European journal of medicinal chemistry, , Nov-29, Volume: 124, 2016
Pyrazolo[1,5-a]-1,3,5-triazine as a purine bioisostere: access to potent cyclin-dependent kinase inhibitor (R)-roscovitine analogue.Journal of medicinal chemistry, , Feb-12, Volume: 52, Issue:3, 2009
Synthesis and biological activity of olomoucine II.Bioorganic & medicinal chemistry letters, , Nov-18, Volume: 12, Issue:22, 2002
Structural classification of protein kinases using 3D molecular interaction field analysis of their ligand binding sites: target family landscapes.Journal of medicinal chemistry, , Jun-06, Volume: 45, Issue:12, 2002
Cyclin-dependent kinase inhibition by new C-2 alkynylated purine derivatives and molecular structure of a CDK2-inhibitor complex.Journal of medicinal chemistry, , Apr-06, Volume: 43, Issue:7, 2000
Exploiting chemical libraries, structure, and genomics in the search for kinase inhibitors.Science (New York, N.Y.), , Jul-24, Volume: 281, Issue:5376, 1998
How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases?Journal of medicinal chemistry, , 10-25, Volume: 61, Issue:20, 2018
Cyclin-dependent kinase inhibitors: useful targets in cell cycle regulation.Journal of medicinal chemistry, , Jan-13, Volume: 43, Issue:1, 2000
How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases?Journal of medicinal chemistry, , 10-25, Volume: 61, Issue:20, 2018
A triple exon-skipping luciferase reporter assay identifies a new CLK inhibitor pharmacophore.Bioorganic & medicinal chemistry letters, , 02-01, Volume: 27, Issue:3, 2017
Recent Developments in the Biology and Medicinal Chemistry of CDK9 Inhibitors: An Update.Journal of medicinal chemistry, , 11-25, Volume: 63, Issue:22, 2020
Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy.Journal of medicinal chemistry, , 10-13, Volume: 59, Issue:19, 2016
Discovery of 8-cyclopentyl-2-[4-(4-methyl-piperazin-1-yl)-phenylamino]-7-oxo-7,8-dihydro-pyrido[2,3-d]pyrimidine-6-carbonitrile (7x) as a potent inhibitor of cyclin-dependent kinase 4 (CDK4) and AMPK-related kinase 5 (ARK5).Journal of medicinal chemistry, , Feb-13, Volume: 57, Issue:3, 2014
A diaminocyclohexyl analog of SNS-032 with improved permeability and bioavailability properties.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 18, Issue:21, 2008
Modifications of the isonipecotic acid fragment of SNS-032: analogs with improved permeability and lower efflux ratio.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 18, Issue:23, 2008
N-(cycloalkylamino)acyl-2-aminothiazole inhibitors of cyclin-dependent kinase 2. N-[5-[[[5-(1,1-dimethylethyl)-2-oxazolyl]methyl]thio]-2-thiazolyl]-4- piperidinecarboxamide (BMS-387032), a highly efficacious and selective antitumor agent.Journal of medicinal chemistry, , Mar-25, Volume: 47, Issue:7, 2004
Development of 5-benzylpaullones and paullone-9-carboxylic acid alkyl esters as selective inhibitors of mitochondrial malate dehydrogenase (mMDH).European journal of medicinal chemistry, , Volume: 45, Issue:1, 2010
Evaluation and comparison of 3D-QSAR CoMSIA models for CDK1, CDK5, and GSK-3 inhibition by paullones.Journal of medicinal chemistry, , Jan-01, Volume: 47, Issue:1, 2004
Pharmacological inhibitors of glycogen synthase kinase 3.Trends in pharmacological sciences, , Volume: 25, Issue:9, 2004
Cyclin-dependent kinase inhibitors: useful targets in cell cycle regulation.Journal of medicinal chemistry, , Jan-13, Volume: 43, Issue:1, 2000
Nitrogen-containing flavonoid analogues as CDK1/cyclin B inhibitors: synthesis, SAR analysis, and biological activity.Bioorganic & medicinal chemistry, , Aug-01, Volume: 16, Issue:15, 2008
Crystal structure of a human cyclin-dependent kinase 6 complex with a flavonol inhibitor, fisetin.Journal of medicinal chemistry, , Feb-10, Volume: 48, Issue:3, 2005
Structure-activity relationship studies of flavopiridol analogues.Bioorganic & medicinal chemistry letters, , May-15, Volume: 10, Issue:10, 2000
Current progress and novel strategies that target CDK12 for drug discovery.European journal of medicinal chemistry, , Oct-05, Volume: 240, 2022
Design, synthesis, and biological evaluation of 4-benzoylamino-1H-pyrazole-3-carboxamide derivatives as potent CDK2 inhibitors.European journal of medicinal chemistry, , Apr-05, Volume: 215, 2021
A review on flavones targeting serine/threonine protein kinases for potential anticancer drugs.Bioorganic & medicinal chemistry, , 03-01, Volume: 27, Issue:5, 2019
Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy.Journal of medicinal chemistry, , 10-13, Volume: 59, Issue:19, 2016
Discovery of 8-cyclopentyl-2-[4-(4-methyl-piperazin-1-yl)-phenylamino]-7-oxo-7,8-dihydro-pyrido[2,3-d]pyrimidine-6-carbonitrile (7x) as a potent inhibitor of cyclin-dependent kinase 4 (CDK4) and AMPK-related kinase 5 (ARK5).Journal of medicinal chemistry, , Feb-13, Volume: 57, Issue:3, 2014
Discovery of novel CDK1 inhibitors by combining pharmacophore modeling, QSAR analysis and in silico screening followed by in vitro bioassay.European journal of medicinal chemistry, , Volume: 45, Issue:9, 2010
Nitrogen-containing flavonoid analogues as CDK1/cyclin B inhibitors: synthesis, SAR analysis, and biological activity.Bioorganic & medicinal chemistry, , Aug-01, Volume: 16, Issue:15, 2008
Structure-based design of a new class of highly selective aminoimidazo[1,2-a]pyridine-based inhibitors of cyclin dependent kinases.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 15, Issue:7, 2005
Crystal structure of a human cyclin-dependent kinase 6 complex with a flavonol inhibitor, fisetin.Journal of medicinal chemistry, , Feb-10, Volume: 48, Issue:3, 2005
Synthesis and biological activity of N-aryl-2-aminothiazoles: potent pan inhibitors of cyclin-dependent kinases.Bioorganic & medicinal chemistry letters, , Jun-07, Volume: 14, Issue:11, 2004
Pharmacological inhibitors of glycogen synthase kinase 3.Trends in pharmacological sciences, , Volume: 25, Issue:9, 2004
Evaluation of the first cytostatically active 1-aza-9-oxafluorenes as novel selective CDK1 inhibitors with P-glycoprotein modulating properties.Journal of medicinal chemistry, , Feb-27, Volume: 46, Issue:5, 2003
1H-Pyrazolo[3,4-b]pyridine inhibitors of cyclin-dependent kinases.Bioorganic & medicinal chemistry letters, , Mar-24, Volume: 13, Issue:6, 2003
Discovery of aminothiazole inhibitors of cyclin-dependent kinase 2: synthesis, X-ray crystallographic analysis, and biological activities.Journal of medicinal chemistry, , Aug-29, Volume: 45, Issue:18, 2002
Structure-activity relationship studies of flavopiridol analogues.Bioorganic & medicinal chemistry letters, , May-15, Volume: 10, Issue:10, 2000
Cyclin-dependent kinase inhibitors: useful targets in cell cycle regulation.Journal of medicinal chemistry, , Jan-13, Volume: 43, Issue:1, 2000
Thio- and oxoflavopiridols, cyclin-dependent kinase 1-selective inhibitors: synthesis and biological effects.Journal of medicinal chemistry, , Nov-02, Volume: 43, Issue:22, 2000
How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases?Journal of medicinal chemistry, , 10-25, Volume: 61, Issue:20, 2018
Aryl[a]pyrrolo[3,4-c]carbazoles as selective cyclin D1-CDK4 inhibitors.Bioorganic & medicinal chemistry letters, , Nov-03, Volume: 13, Issue:21, 2003
Synthesis, structure-activity relationship, and biological studies of indolocarbazoles as potent cyclin D1-CDK4 inhibitors.Journal of medicinal chemistry, , May-22, Volume: 46, Issue:11, 2003
Discovery of a novel series of imidazo[1',2':1,6]pyrido[2,3-d]pyrimidin derivatives as potent cyclin-dependent kinase 4/6 inhibitors.European journal of medicinal chemistry, , May-01, Volume: 193, 2020
[no title available]European journal of medicinal chemistry, , Mar-01, Volume: 165, 2019
How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases?Journal of medicinal chemistry, , 10-25, Volume: 61, Issue:20, 2018
Highly Potent, Selective, and Orally Bioavailable 4-Thiazol-N-(pyridin-2-yl)pyrimidin-2-amine Cyclin-Dependent Kinases 4 and 6 Inhibitors as Anticancer Drug Candidates: Design, Synthesis, and Evaluation.Journal of medicinal chemistry, , 03-09, Volume: 60, Issue:5, 2017
Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy.Journal of medicinal chemistry, , 10-13, Volume: 59, Issue:19, 2016
Indole-fused azepines and analogues as anticancer lead molecules: Privileged findings and future directions.European journal of medicinal chemistry, , Dec-15, Volume: 142, 2017
1-Azakenpaullone is a selective inhibitor of glycogen synthase kinase-3 beta.Bioorganic & medicinal chemistry letters, , Jan-19, Volume: 14, Issue:2, 2004
Pharmacological inhibitors of glycogen synthase kinase 3.Trends in pharmacological sciences, , Volume: 25, Issue:9, 2004
Design, synthesis, and biological evaluation of 4-benzoylamino-1H-pyrazole-3-carboxamide derivatives as potent CDK2 inhibitors.European journal of medicinal chemistry, , Apr-05, Volume: 215, 2021
Cyclin-Dependent Kinase 2 Inhibitors in Cancer Therapy: An Update.Journal of medicinal chemistry, , 05-09, Volume: 62, Issue:9, 2019
Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy.Journal of medicinal chemistry, , 10-13, Volume: 59, Issue:19, 2016
Cyclin dependent kinase (CDK) inhibitors as anticancer drugs.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 25, Issue:17, 2015
Identification of N-(4-piperidinyl)-4-(2,6-dichlorobenzoylamino)-1H-pyrazole-3-carboxamide (AT7519), a novel cyclin dependent kinase inhibitor using fragment-based X-ray crystallography and structure based drug design.Journal of medicinal chemistry, , Aug-28, Volume: 51, Issue:16, 2008
Discovery of a Pyrimidothiazolodiazepinone as a Potent and Selective Focal Adhesion Kinase (FAK) Inhibitor.ACS medicinal chemistry letters, , Jan-14, Volume: 12, Issue:1, 2021
Cellular characterization of a novel focal adhesion kinase inhibitor.The Journal of biological chemistry, , May-18, Volume: 282, Issue:20, 2007
Cyclin-Dependent Kinase 2 Inhibitors in Cancer Therapy: An Update.Journal of medicinal chemistry, , 05-09, Volume: 62, Issue:9, 2019
How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases?Journal of medicinal chemistry, , 10-25, Volume: 61, Issue:20, 2018
Identification of N,1,4,4-tetramethyl-8-{[4-(4-methylpiperazin-1-yl)phenyl]amino}-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide (PHA-848125), a potent, orally available cyclin dependent kinase inhibitor.Journal of medicinal chemistry, , Aug-27, Volume: 52, Issue:16, 2009
Optimization of pyrazolo[1,5-a]pyrimidines lead to the identification of a highly selective casein kinase 2 inhibitor.European journal of medicinal chemistry, , Dec-15, Volume: 208, 2020
Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer.Journal of medicinal chemistry, , Jan-27, Volume: 54, Issue:2, 2011
How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases?Journal of medicinal chemistry, , 10-25, Volume: 61, Issue:20, 2018
Discovery of 8-cyclopentyl-2-[4-(4-methyl-piperazin-1-yl)-phenylamino]-7-oxo-7,8-dihydro-pyrido[2,3-d]pyrimidine-6-carbonitrile (7x) as a potent inhibitor of cyclin-dependent kinase 4 (CDK4) and AMPK-related kinase 5 (ARK5).Journal of medicinal chemistry, , Feb-13, Volume: 57, Issue:3, 2014
How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases?Journal of medicinal chemistry, , 10-25, Volume: 61, Issue:20, 2018
Potent inhibitors of CDK5 derived from roscovitine: synthesis, biological evaluation and molecular modelling.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 23, Issue:1, 2013
Design, synthesis, and biological evaluation of 4-benzoylamino-1H-pyrazole-3-carboxamide derivatives as potent CDK2 inhibitors.European journal of medicinal chemistry, , Apr-05, Volume: 215, 2021
How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases?Journal of medicinal chemistry, , 10-25, Volume: 61, Issue:20, 2018
Cyclin-Dependent Kinase 2 Inhibitors in Cancer Therapy: An Update.Journal of medicinal chemistry, , 05-09, Volume: 62, Issue:9, 2019
Recent development of CDK inhibitors: An overview of CDK/inhibitor co-crystal structures.European journal of medicinal chemistry, , Feb-15, Volume: 164, 2019
Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy.Journal of medicinal chemistry, , 10-13, Volume: 59, Issue:19, 2016
Cyclin dependent kinase (CDK) inhibitors as anticancer drugs.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 25, Issue:17, 2015
Design, synthesis, and biological evaluation of 4-benzoylamino-1H-pyrazole-3-carboxamide derivatives as potent CDK2 inhibitors.European journal of medicinal chemistry, , Apr-05, Volume: 215, 2021
Discovery of a novel series of imidazo[1',2':1,6]pyrido[2,3-d]pyrimidin derivatives as potent cyclin-dependent kinase 4/6 inhibitors.European journal of medicinal chemistry, , May-01, Volume: 193, 2020
Design, synthesis and biological evaluation of tetrahydronaphthyridine derivatives as bioavailable CDK4/6 inhibitors for cancer therapy.European journal of medicinal chemistry, , Mar-25, Volume: 148, 2018
How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases?Journal of medicinal chemistry, , 10-25, Volume: 61, Issue:20, 2018
Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy.Journal of medicinal chemistry, , 10-13, Volume: 59, Issue:19, 2016
Synthesis, biological evaluation and molecular modeling of a novel series of 7-azaindole based tri-heterocyclic compounds as potent CDK2/Cyclin E inhibitors.European journal of medicinal chemistry, , Jan-27, Volume: 108, 2016
Cyclin dependent kinase (CDK) inhibitors as anticancer drugs.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 25, Issue:17, 2015
3,5,7-Substituted Pyrazolo[4,3- d]pyrimidine Inhibitors of Cyclin-Dependent Kinases and Their Evaluation in Lymphoma Models.Journal of medicinal chemistry, , 05-09, Volume: 62, Issue:9, 2019
Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy.Journal of medicinal chemistry, , 10-13, Volume: 59, Issue:19, 2016
Synthesis, biological evaluation and molecular modeling of a novel series of 7-azaindole based tri-heterocyclic compounds as potent CDK2/Cyclin E inhibitors.European journal of medicinal chemistry, , Jan-27, Volume: 108, 2016
Discovery of novel CDK1 inhibitors by combining pharmacophore modeling, QSAR analysis and in silico screening followed by in vitro bioassay.European journal of medicinal chemistry, , Volume: 45, Issue:9, 2010
Thio- and oxoflavopiridols, cyclin-dependent kinase 1-selective inhibitors: synthesis and biological effects.Journal of medicinal chemistry, , Nov-02, Volume: 43, Issue:22, 2000
Novel arylazopyrazole inhibitors of cyclin-dependent kinases.Bioorganic & medicinal chemistry, , May-01, Volume: 23, Issue:9, 2015
4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects.Journal of medicinal chemistry, , Nov-02, Volume: 49, Issue:22, 2006
Synthesis and evaluation of novel anti-proliferative pyrroloazepinone and indoloazepinone oximes derived from the marine natural product hymenialdisine.European journal of medicinal chemistry, , Volume: 56, 2012
1-Azakenpaullone is a selective inhibitor of glycogen synthase kinase-3 beta.Bioorganic & medicinal chemistry letters, , Jan-19, Volume: 14, Issue:2, 2004
Pharmacological inhibitors of glycogen synthase kinase 3.Trends in pharmacological sciences, , Volume: 25, Issue:9, 2004
Enables
This protein enables 6 target(s):
| Target | Category | Definition |
|---|
| patched binding | molecular function | Binding to a patched (ptc) protein, a receptor for hedgehog proteins. [GOC:ceb, PMID:11731473] |
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| protein kinase binding | molecular function | Binding to a protein kinase, any enzyme that catalyzes the transfer of a phosphate group, usually from ATP, to a protein substrate. [GOC:jl] |
| ubiquitin-like protein ligase binding | molecular function | Binding to a ubiquitin-like protein ligase, such as ubiquitin-ligase. [GOC:jl] |
| cyclin-dependent protein serine/threonine kinase activator activity | molecular function | Binds to and increases the activity of a cyclin-dependent protein serine/threonine kinase. [GOC:dph, PMID:2569363, PMID:3322810] |
| cyclin-dependent protein serine/threonine kinase regulator activity | molecular function | Modulates the activity of a cyclin-dependent protein serine/threonine kinase, enzymes of the protein kinase family that are regulated through association with cyclins and other proteins. [GOC:pr, GOC:rn, PMID:7877684, PMID:9442875] |
Located In
This protein is located in 7 target(s):
| Target | Category | Definition |
|---|
| spindle pole | cellular component | Either of the ends of a spindle, where spindle microtubules are organized; usually contains a microtubule organizing center and accessory molecules, spindle microtubules and astral microtubules. [GOC:clt] |
| nucleus | cellular component | A membrane-bounded organelle of eukaryotic cells in which chromosomes are housed and replicated. In most cells, the nucleus contains all of the cell's chromosomes except the organellar chromosomes, and is the site of RNA synthesis and processing. In some species, or in specialized cell types, RNA metabolism or DNA replication may be absent. [GOC:go_curators] |
| nucleoplasm | cellular component | That part of the nuclear content other than the chromosomes or the nucleolus. [GOC:ma, ISBN:0124325653] |
| cytoplasm | cellular component | The contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684] |
| centrosome | cellular component | A structure comprised of a core structure (in most organisms, a pair of centrioles) and peripheral material from which a microtubule-based structure, such as a spindle apparatus, is organized. Centrosomes occur close to the nucleus during interphase in many eukaryotic cells, though in animal cells it changes continually during the cell-division cycle. [GOC:mah, ISBN:0198547684] |
| cytosol | cellular component | The part of the cytoplasm that does not contain organelles but which does contain other particulate matter, such as protein complexes. [GOC:hjd, GOC:jl] |
| membrane | cellular component | A lipid bilayer along with all the proteins and protein complexes embedded in it and attached to it. [GOC:dos, GOC:mah, ISBN:0815316194] |
Active In
This protein is active in 3 target(s):
| Target | Category | Definition |
|---|
| cytoplasm | cellular component | The contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684] |
| nucleus | cellular component | A membrane-bounded organelle of eukaryotic cells in which chromosomes are housed and replicated. In most cells, the nucleus contains all of the cell's chromosomes except the organellar chromosomes, and is the site of RNA synthesis and processing. In some species, or in specialized cell types, RNA metabolism or DNA replication may be absent. [GOC:go_curators] |
| centrosome | cellular component | A structure comprised of a core structure (in most organisms, a pair of centrioles) and peripheral material from which a microtubule-based structure, such as a spindle apparatus, is organized. Centrosomes occur close to the nucleus during interphase in many eukaryotic cells, though in animal cells it changes continually during the cell-division cycle. [GOC:mah, ISBN:0198547684] |
Part Of
This protein is part of 2 target(s):
| Target | Category | Definition |
|---|
| cyclin B1-CDK1 complex | cellular component | A protein complex consisting of cyclin B1 and cyclin-dependent kinase 1 (CDK1). Cyclins are characterized by periodicity in protein abundance throughout the cell cycle. Cyclin-dependent kinases represent a family of serine/threonine protein kinases that become active upon binding to a cyclin regulatory partner. [GOC:so, PMID:15935619] |
| outer kinetochore | cellular component | The region of a kinetochore most external to centromeric DNA; this outer region mediates kinetochore-microtubule interactions. [GOC:clt, PMID:11483983] |
Involved In
This protein is involved in 13 target(s):
| Target | Category | Definition |
|---|
| G2/M transition of mitotic cell cycle | biological process | The mitotic cell cycle transition by which a cell in G2 commits to M phase. The process begins when the kinase activity of M cyclin/CDK complex reaches a threshold high enough for the cell cycle to proceed. This is accomplished by activating a positive feedback loop that results in the accumulation of unphosphorylated and active M cyclin/CDK complex. [GOC:mtg_cell_cycle] |
| in utero embryonic development | biological process | The process whose specific outcome is the progression of the embryo in the uterus over time, from formation of the zygote in the oviduct, to birth. An example of this process is found in Mus musculus. [GOC:go_curators, GOC:mtg_sensu] |
| mitotic spindle organization | biological process | A process that is carried out at the cellular level which results in the assembly, arrangement of constituent parts, or disassembly of the microtubule spindle during a mitotic cell cycle. [GOC:go_curators, GOC:mah] |
| mitotic metaphase chromosome alignment | biological process | A chromosome localization process whereby chromosomes are positioned in a specific order and orientation at the metaphase plate (spindle equator), during mitotic chromosome segregation. This alignment ensures that each daughter cell will receive the correct number of chromosomes during cell division. [ISBN:0815316194] |
| positive regulation of G2/M transition of mitotic cell cycle | biological process | Any signaling pathway that activates or increases the activity of a cell cycle cyclin-dependent protein kinase to modulate the switch from G2 phase to M phase of the mitotic cell cycle. [GOC:dph, GOC:mtg_cell_cycle, GOC:tb] |
| positive regulation of mitotic cell cycle | biological process | Any process that activates or increases the rate or extent of progression through the mitotic cell cycle. [GOC:dph, GOC:go_curators, GOC:tb] |
| positive regulation of fibroblast proliferation | biological process | Any process that activates or increases the frequency, rate or extent of multiplication or reproduction of fibroblast cells. [GOC:jid] |
| cell division | biological process | The process resulting in division and partitioning of components of a cell to form more cells; may or may not be accompanied by the physical separation of a cell into distinct, individually membrane-bounded daughter cells. [GOC:di, GOC:go_curators, GOC:pr] |
| positive regulation of attachment of spindle microtubules to kinetochore | biological process | Any process that activates or increases the frequency, rate or extent of the attachment of spindle microtubules to the kinetochore. [GOC:ai] |
| regulation of mitotic cell cycle spindle assembly checkpoint | biological process | Any process that modulates the rate, frequency, or extent of the mitotic cell cycle spindle assembly checkpoint, a cell cycle checkpoint that delays the metaphase/anaphase transition of a mitotic nuclear division until the spindle is correctly assembled and chromosomes are attached to the spindle. [GOC:mtg_cell_cycle] |
| positive regulation of mitochondrial ATP synthesis coupled electron transport | biological process | Any process that activates or increases the frequency, rate or extent of mitochondrial ATP synthesis coupled electron transport. [GO_REF:0000058, GOC:bc, GOC:PARL, GOC:TermGenie, PMID:23707074] |
| regulation of cyclin-dependent protein serine/threonine kinase activity | biological process | Any process that modulates the frequency, rate or extent of cyclin-dependent protein serine/threonine kinase activity. [GOC:go_curators, GOC:pr] |
| mitotic cell cycle phase transition | biological process | The cell cycle process by which a cell commits to entering the next mitotic cell cycle phase. [GOC:mtg_cell_cycle] |