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G1/S-specific cyclin-E1
A G1/S-specific cyclin-E1 that is encoded in the genome of human. [PRO:DNx]
Synonyms
Research
Bioassay Publications (84)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 28 (33.33) | 29.6817 |
| 2010's | 45 (53.57) | 24.3611 |
| 2020's | 11 (13.10) | 2.80 |
Compounds (72)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| tyrphostin a23 | Homo sapiens (human) | Ki | 0.6166 | 1 | 1 |
| bisindolylmaleimide i | Homo sapiens (human) | IC50 | 12.2700 | 2 | 5 |
| bisindolylmaleimide iv | Homo sapiens (human) | IC50 | 12.2975 | 2 | 4 |
| bohemine | Homo sapiens (human) | IC50 | 1.6500 | 1 | 2 |
| n(6),n(6)-dimethyladenine | Homo sapiens (human) | Ki | 1.0965 | 1 | 1 |
| gw8510 | Homo sapiens (human) | IC50 | 0.0030 | 1 | 1 |
| indirubin-3'-monoxime | Homo sapiens (human) | IC50 | 0.7000 | 1 | 1 |
| staurosporine aglycone | Homo sapiens (human) | IC50 | 0.9433 | 3 | 3 |
| nu6102 | Homo sapiens (human) | IC50 | 0.0335 | 2 | 2 |
| nu6102 | Homo sapiens (human) | Ki | 0.0010 | 1 | 1 |
| olomoucine | Homo sapiens (human) | IC50 | 89.2400 | 9 | 12 |
| imatinib | Homo sapiens (human) | IC50 | 77.5000 | 4 | 4 |
| indirubin | Homo sapiens (human) | IC50 | 4.8500 | 2 | 2 |
| indigo | Homo sapiens (human) | IC50 | 1.0000 | 1 | 1 |
| staurosporine | Homo sapiens (human) | IC50 | 0.0108 | 17 | 17 |
| fascaplysine | Homo sapiens (human) | IC50 | 250.0000 | 1 | 1 |
| LSM-4272 | Homo sapiens (human) | IC50 | 25.1750 | 1 | 2 |
| dehydroabietic acid | Homo sapiens (human) | IC50 | 36.2900 | 1 | 1 |
| birb 796 | Homo sapiens (human) | IC50 | 30.0000 | 1 | 1 |
| cyc 202 | Homo sapiens (human) | IC50 | 4.6708 | 25 | 30 |
| lapatinib | Homo sapiens (human) | IC50 | 20.0000 | 1 | 1 |
| 2H-pyrazolo[4,3-b]quinoxalin-3-amine | Homo sapiens (human) | IC50 | 5.6000 | 1 | 1 |
| 7-n-butyl-6-(4'-hydroxyphenyl)-5h-pyrrolo(2,3b)pyrazine | Homo sapiens (human) | IC50 | 0.4000 | 1 | 1 |
| 6-bromoindirubin-3'-oxime | Homo sapiens (human) | IC50 | 0.0140 | 1 | 1 |
| purvalanol b | Homo sapiens (human) | IC50 | 0.0090 | 1 | 1 |
| repsox | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| purvalanol a | Homo sapiens (human) | IC50 | 0.0350 | 1 | 1 |
| 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 | 0.0030 | 1 | 1 |
| cgp 74514a | Homo sapiens (human) | IC50 | 0.0215 | 2 | 2 |
| 1,4-dimethoxy-10H-acridine-9-thione | Homo sapiens (human) | IC50 | 40.0667 | 2 | 3 |
| bms 387032 | Homo sapiens (human) | IC50 | 8.0383 | 6 | 6 |
| sf 2370 | Homo sapiens (human) | IC50 | 0.1450 | 1 | 2 |
| sb 218078 | Homo sapiens (human) | IC50 | 0.6333 | 2 | 3 |
| 7-butyl-6-(4-methoxyphenyl)-5H-pyrrolo[2,3-b]pyrazine | Homo sapiens (human) | Ki | 0.0005 | 1 | 1 |
| alvocidib | Homo sapiens (human) | IC50 | 15.2146 | 16 | 22 |
| aftin-4 | Homo sapiens (human) | IC50 | 556.6667 | 1 | 6 |
| su 9516 | Homo sapiens (human) | IC50 | 5.8532 | 2 | 5 |
| arcyriaflavin a | Homo sapiens (human) | IC50 | 1.8697 | 8 | 16 |
| pd 0183812 | Homo sapiens (human) | IC50 | 8.1094 | 2 | 5 |
| palbociclib | Homo sapiens (human) | IC50 | 9.1500 | 2 | 2 |
| olomoucine ii | Homo sapiens (human) | IC50 | 0.0500 | 1 | 1 |
| cyc 116 | Homo sapiens (human) | IC50 | 1.7000 | 1 | 2 |
| cyc 116 | Homo sapiens (human) | Ki | 0.3900 | 1 | 1 |
| 2-[[6-[(phenylmethyl)amino]-9-propan-2-yl-2-purinyl]amino]ethanol | Homo sapiens (human) | IC50 | 8.7000 | 1 | 2 |
| cvt 313 | Homo sapiens (human) | IC50 | 0.1760 | 1 | 1 |
| ((3z)-n-(3-chlorophenyl)-3-((3,5-dimethyl-4-((4-methylpiperazin-1-yl)carbonyl)-1h-pyrrol-2-yl)methylene)-n-methyl-2-oxo-2,3-dihydro-1h-indole-5-sulfonamide) | Homo sapiens (human) | Ki | 0.4898 | 1 | 1 |
| azd2858 | Homo sapiens (human) | Ki | 0.5400 | 1 | 1 |
| nu 6140 | Homo sapiens (human) | IC50 | 1.1000 | 1 | 1 |
| rgb 286638 | Homo sapiens (human) | IC50 | 0.0020 | 2 | 2 |
| at 7519 | Homo sapiens (human) | IC50 | 0.3600 | 3 | 3 |
| at 7519 | Homo sapiens (human) | Ki | 0.5100 | 1 | 1 |
| pha 848125 | Homo sapiens (human) | IC50 | 0.3881 | 3 | 7 |
| 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 | 0.0060 | 4 | 4 |
| azd5438 | Homo sapiens (human) | IC50 | 0.0060 | 1 | 1 |
| p276-00 | Homo sapiens (human) | IC50 | 2.6700 | 2 | 2 |
| cx 4945 | Homo sapiens (human) | IC50 | 1.8000 | 1 | 1 |
| bms 754807 | Homo sapiens (human) | IC50 | 1.0350 | 1 | 1 |
| pci 32765 | Homo sapiens (human) | IC50 | 25.0000 | 1 | 1 |
| cink4 | Homo sapiens (human) | IC50 | 27.6000 | 2 | 2 |
| bs 194 | Homo sapiens (human) | IC50 | 0.0030 | 1 | 1 |
| (R)-DRF053 | Homo sapiens (human) | IC50 | 0.0930 | 1 | 1 |
| ribociclib | Homo sapiens (human) | IC50 | 20.0000 | 3 | 3 |
| bay 1000394 | Homo sapiens (human) | IC50 | 0.0092 | 5 | 5 |
| pha 793887 | Homo sapiens (human) | IC50 | 0.0080 | 1 | 1 |
| abemaciclib | Homo sapiens (human) | IC50 | 0.2320 | 3 | 3 |
| abemaciclib | Homo sapiens (human) | Ki | 0.5040 | 1 | 1 |
| dinaciclib | Homo sapiens (human) | IC50 | 0.0028 | 4 | 4 |
| nms p937 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| gilteritinib | Homo sapiens (human) | Ki | 1.4850 | 1 | 1 |
| bs-181 | Homo sapiens (human) | IC50 | 1.8000 | 1 | 1 |
| butyrolactone i | Homo sapiens (human) | IC50 | 1.5000 | 1 | 1 |
| on123300 | Homo sapiens (human) | IC50 | 0.3770 | 1 | 1 |
| can 508 | Homo sapiens (human) | IC50 | 23.6350 | 5 | 10 |
| can 508 | Homo sapiens (human) | Ki | 13.3000 | 1 | 1 |
| ro 3306 | Homo sapiens (human) | IC50 | 0.1860 | 1 | 1 |
| hymenialdisine | Homo sapiens (human) | IC50 | 0.0400 | 1 | 1 |
Drugs with Other Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| olomoucine | Homo sapiens (human) | ID50 | 7.0000 | 1 | 1 |
| purvalanol b | Homo sapiens (human) | ID50 | 0.0090 | 1 | 1 |
| cgp 60474 | Homo sapiens (human) | ID50 | 0.0500 | 1 | 1 |
Aryl[a]pyrrolo[3,4-c]carbazoles as selective cyclin D1-CDK4 inhibitors.Bioorganic & medicinal chemistry letters, , Nov-03, Volume: 13, Issue:21, 2003
Studies on cyclin-dependent kinase inhibitors: indolo-[2,3-a]pyrrolo[3,4-c]carbazoles versus bis-indolylmaleimides.Bioorganic & medicinal chemistry letters, , Nov-03, Volume: 13, Issue:21, 2003
Recent development of CDK inhibitors: An overview of CDK/inhibitor co-crystal structures.European journal of medicinal chemistry, , Feb-15, Volume: 164, 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 binding specificity-determining features in protein families.Journal of medicinal chemistry, , Mar-08, Volume: 55, Issue:5, 2012
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
Synthesis, biological evaluation, and molecular docking studies of N-((1,3-diphenyl-1H-pyrazol-4-yl)methyl)aniline derivatives as novel anticancer agents.Bioorganic & medicinal chemistry, , Aug-15, Volume: 20, Issue:16, 2012
Biaryl purine derivatives as potent antiproliferative agents: inhibitors of cyclin dependent kinases. Part I.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 19, Issue:23, 2009
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
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
Cinnamaldehydes inhibit cyclin dependent kinase 4/cyclin D1.Bioorganic & medicinal chemistry letters, , Aug-21, Volume: 10, Issue:16, 2000
Docking-based development of purine-like inhibitors of cyclin-dependent kinase-2.Journal of medicinal chemistry, , Jun-29, Volume: 43, Issue:13, 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
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
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
New approaches to the synthesis of sildenafil analogues and their enzyme inhibitory activity.Bioorganic & medicinal chemistry, , Apr-01, Volume: 23, Issue:7, 2015
Synthesis and kinase inhibitory activity of new sulfonamide derivatives of pyrazolo[4,3-e][1,2,4]triazines.European journal of medicinal chemistry, , May-06, Volume: 78, 2014
Design, synthesis and biological evaluation of pteridine-7(8H)-one derivatives as potent and selective CDK4/6 inhibitors.Bioorganic & medicinal chemistry letters, , 11-15, Volume: 76, 2022
Tetrahydroindazole inhibitors of CDK2/cyclin complexes.European journal of medicinal chemistry, , Mar-15, Volume: 214, 2021
Discovery of a 2-pyridinyl urea-containing compound YD57 as a potent inhibitor of apoptosis signal-regulating kinase 1 (ASK1).European journal of medicinal chemistry, , Jun-01, Volume: 195, 2020
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
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
Development of highly potent and selective diaminothiazole inhibitors of cyclin-dependent kinases.Journal of medicinal chemistry, , May-23, Volume: 56, Issue:10, 2013
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
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
Aryl[a]pyrrolo[3,4-c]carbazoles as selective cyclin D1-CDK4 inhibitors.Bioorganic & medicinal chemistry letters, , Nov-03, Volume: 13, Issue:21, 2003
Novel, potent and selective cyclin D1/CDK4 inhibitors: indolo[6,7-a]pyrrolo[3,4-c]carbazoles.Bioorganic & medicinal chemistry letters, , Jul-21, Volume: 13, Issue:14, 2003
[no title available]Journal of medicinal chemistry, , 07-14, Volume: 65, Issue:13, 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
CDK7 Inhibitors in Cancer Therapy: The Sweet Smell of Success?Journal of medicinal chemistry, , 07-23, Volume: 63, Issue:14, 2020
Sulfonamide-based ring-fused analogues for CAN508 as novel carbonic anhydrase inhibitors endowed with antitumor activity: Design, synthesis, and in vitro biological evaluation.European journal of medicinal chemistry, , Mar-01, Volume: 189, 2020
Cyclin dependent kinase (CDK) inhibitors as anticancer drugs: Recent advances (2015-2019).Bioorganic & medicinal chemistry letters, , 10-15, Volume: 29, Issue:20, 2019
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
5-Substituted 3-isopropyl-7-[4-(2-pyridyl)benzyl]amino-1(2)H-pyrazolo[4,3-d]pyrimidines with anti-proliferative activity as potent and selective inhibitors of cyclin-dependent kinases.European journal of medicinal chemistry, , Mar-03, Volume: 110, 2016
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
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
New approaches to the synthesis of sildenafil analogues and their enzyme inhibitory activity.Bioorganic & medicinal chemistry, , Apr-01, Volume: 23, Issue:7, 2015
Synthesis and kinase inhibitory activity of new sulfonamide derivatives of pyrazolo[4,3-e][1,2,4]triazines.European journal of medicinal chemistry, , May-06, Volume: 78, 2014
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
Synthesis and in vitro biological evaluation of 2,6,9-trisubstituted purines targeting multiple cyclin-dependent kinases.European journal of medicinal chemistry, , Volume: 61, 2013
Synthesis and biological evaluation of guanidino analogues of roscovitine.European journal of medicinal chemistry, , Volume: 62, 2013
A novel series of highly potent 2,6,9-trisubstituted purine cyclin-dependent kinase inhibitors.Journal of medicinal chemistry, , Aug-08, Volume: 56, Issue:15, 2013
Pyrazolo[4,3-d]pyrimidine bioisostere of roscovitine: evaluation of a novel selective inhibitor of cyclin-dependent kinases with antiproliferative activity.Journal of medicinal chemistry, , Apr-28, Volume: 54, Issue:8, 2011
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
Biaryl purine derivatives as potent antiproliferative agents: inhibitors of cyclin dependent kinases. Part I.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 19, Issue:23, 2009
Heterobiaryl purine derivatives as potent antiproliferative agents: inhibitors of cyclin dependent kinases. Part II.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 19, Issue:23, 2009
Crystal structure of pyridoxal kinase in complex with roscovitine and derivatives.The Journal of biological chemistry, , Sep-02, Volume: 280, Issue:35, 2005
Seliciclib (CYC202, R-Roscovitine) induces cell death in multiple myeloma cells by inhibition of RNA polymerase II-dependent transcription and down-regulation of Mcl-1.Cancer research, , Jun-15, Volume: 65, Issue:12, 2005
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
Crystal structure of human cyclin-dependent kinase 2 in complex with the adenine-derived inhibitor H717.Journal of medicinal chemistry, , Feb-15, Volume: 44, Issue:4, 2001
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 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
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
Trisubstituted purine inhibitors of PDGFRα and their antileukemic activity in the human eosinophilic cell line EOL-1.Bioorganic & medicinal chemistry, , 12-15, Volume: 25, Issue:24, 2017
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
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
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
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
[no title available]MedChemComm, , Mar-01, Volume: 6, Issue:3, 2015
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
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
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
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
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
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
Novel pyrrolyllactone and pyrrolyllactam indolinones as potent cyclin-dependent kinase 2 inhibitors.Bioorganic & medicinal chemistry letters, , Jun-02, Volume: 13, Issue:11, 2003
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
Studies on cyclin-dependent kinase inhibitors: indolo-[2,3-a]pyrrolo[3,4-c]carbazoles versus bis-indolylmaleimides.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
Novel, potent and selective cyclin D1/CDK4 inhibitors: indolo[6,7-a]pyrrolo[3,4-c]carbazoles.Bioorganic & medicinal chemistry letters, , Jul-21, Volume: 13, Issue:14, 2003
How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases?Journal of medicinal chemistry, , 10-25, Volume: 61, Issue:20, 2018
5-Substituted 3-isopropyl-7-[4-(2-pyridyl)benzyl]amino-1(2)H-pyrazolo[4,3-d]pyrimidines with anti-proliferative activity as potent and selective inhibitors of cyclin-dependent kinases.European journal of medicinal chemistry, , Mar-03, Volume: 110, 2016
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 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
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 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
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
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
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
First orally bioavailable prodrug of proteolysis targeting chimera (PROTAC) degrades cyclin-dependent kinases 2/4/6 in vivo.European journal of medicinal chemistry, , Jan-01, Volume: 209, 2021
How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases?Journal of medicinal chemistry, , 10-25, Volume: 61, Issue:20, 2018
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 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
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
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
[no title available]Journal of medicinal chemistry, , 07-14, Volume: 65, Issue:13, 2022
Imidazo[1,2-c]pyrimidin-5(6H)-one inhibitors of CDK2: Synthesis, kinase inhibition and co-crystal structure.European journal of medicinal chemistry, , Apr-15, Volume: 216, 2021
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
5-Substituted 3-isopropyl-7-[4-(2-pyridyl)benzyl]amino-1(2)H-pyrazolo[4,3-d]pyrimidines with anti-proliferative activity as potent and selective inhibitors of cyclin-dependent kinases.European journal of medicinal chemistry, , Mar-03, Volume: 110, 2016
Sulfonamide-based ring-fused analogues for CAN508 as novel carbonic anhydrase inhibitors endowed with antitumor activity: Design, synthesis, and in vitro biological evaluation.European journal of medicinal chemistry, , Mar-01, Volume: 189, 2020
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
Enables
This protein enables 4 target(s):
| Target | Category | Definition |
|---|
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| kinase activity | molecular function | Catalysis of the transfer of a phosphate group, usually from ATP, to a substrate molecule. [ISBN:0198506732] |
| 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] |
| 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 3 target(s):
| Target | Category | Definition |
|---|
| 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] |
| 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] |
Active In
This protein is active in 3 target(s):
| Target | Category | Definition |
|---|
| 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] |
| 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] |
| cytoplasm | cellular component | The contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684] |
Part Of
This protein is part of 1 target(s):
| Target | Category | Definition |
|---|
| cyclin E1-CDK2 complex | cellular component | A protein complex consisting of cyclin E1 and cyclin-dependent kinase 2 (CDK2). 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] |
Involved In
This protein is involved in 11 target(s):
| Target | Category | Definition |
|---|
| G1/S transition of mitotic cell cycle | biological process | The mitotic cell cycle transition by which a cell in G1 commits to S phase. The process begins with the build up of G1 cyclin-dependent kinase (G1 CDK), resulting in the activation of transcription of G1 cyclins. The process ends with the positive feedback of the G1 cyclins on the G1 CDK which commits the cell to S phase, in which DNA replication is initiated. [GOC:mtg_cell_cycle] |
| negative regulation of transcription by RNA polymerase II | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of transcription mediated by RNA polymerase II. [GOC:go_curators, GOC:txnOH] |
| telomere maintenance | biological process | Any process that contributes to the maintenance of proper telomeric length and structure by affecting and monitoring the activity of telomeric proteins, the length of telomeric DNA and the replication and repair of the DNA. These processes includes those that shorten, lengthen, replicate and repair the telomeric DNA sequences. [GOC:BHF, GOC:BHF_telomere, GOC:elh, GOC:rl, PMID:11092831] |
| DNA replication initiation | biological process | The process in which DNA-dependent DNA replication is started; it begins when specific sequences, known as origins of replication, are recognized and bound by the origin recognition complex, followed by DNA unwinding. [PMID:28209641] |
| homologous chromosome pairing at meiosis | biological process | The meiotic cell cycle process where side by side pairing and physical juxtaposition of homologous chromosomes is created during meiotic prophase. Homologous chromosome pairing begins when the chromosome arms begin to pair from the clustered telomeres and ends when synaptonemal complex or linear element assembly is complete. [GOC:mtg_cell_cycle, PMID:22582262, PMID:23117617, PMID:31811152] |
| Wnt signaling pathway | biological process | The series of molecular signals initiated by binding of a Wnt protein to a frizzled family receptor on the surface of a target cell and ending with a change in cell state. [PMID:11532397] |
| regulation of protein localization | biological process | Any process that modulates the frequency, rate or extent of any process in which a protein is transported to, or maintained in, a specific location. [GOC:dph, GOC:mah, GOC:tb] |
| 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 mesenchymal stem cell proliferation | biological process | Any process that activates or increases the frequency, rate or extent of mesenchymal stem cell proliferation. [GOC:pm, GOC:TermGenie, PMID:18672106] |
| 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] |
| positive regulation of G1/S transition of mitotic cell cycle | biological process | Any signaling pathway that increases or activates a cell cycle cyclin-dependent protein kinase to modulate the switch from G1 phase to S phase of the mitotic cell cycle. [GOC:mtg_cell_cycle] |