Page last updated: 2024-08-07 16:08:44
Cyclin-A2
A cyclin-A2 that is encoded in the genome of human. [PRO:CNA, UniProtKB:P20248]
Synonyms
Cyclin-A;
Cyclin A
Research
Bioassay Publications (114)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 33 (28.95) | 29.6817 |
| 2010's | 64 (56.14) | 24.3611 |
| 2020's | 17 (14.91) | 2.80 |
Compounds (83)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| 1-anilino-8-naphthalenesulfonate | Homo sapiens (human) | IC50 | 91.0000 | 2 | 2 |
| gw8510 | Homo sapiens (human) | IC50 | 0.0065 | 2 | 2 |
| indirubin-3'-monoxime | Homo sapiens (human) | IC50 | 0.5150 | 2 | 2 |
| indirubin-5-sulfonate | Homo sapiens (human) | IC50 | 0.0350 | 2 | 2 |
| nsc 664704 | Homo sapiens (human) | IC50 | 0.7300 | 2 | 2 |
| nu2058 | Homo sapiens (human) | IC50 | 13.6667 | 4 | 6 |
| nu2058 | Homo sapiens (human) | Ki | 9.6667 | 2 | 3 |
| nu6102 | Homo sapiens (human) | IC50 | 0.1303 | 7 | 15 |
| nu6102 | Homo sapiens (human) | Ki | 0.0060 | 1 | 1 |
| o(6)-benzylguanine | Homo sapiens (human) | IC50 | 29.5000 | 2 | 4 |
| olomoucine | Homo sapiens (human) | IC50 | 7.7500 | 4 | 4 |
| dichlororibofuranosylbenzimidazole | Homo sapiens (human) | Ki | 65.0000 | 1 | 1 |
| indazoles | Homo sapiens (human) | IC50 | 185.0000 | 2 | 2 |
| indirubin | Homo sapiens (human) | IC50 | 3.5250 | 4 | 4 |
| staurosporine | Homo sapiens (human) | IC50 | 4.1749 | 12 | 12 |
| staurosporine | Homo sapiens (human) | Ki | 0.0026 | 2 | 3 |
| 7-hydroxystaurosporine | Homo sapiens (human) | Ki | 0.0625 | 1 | 2 |
| fascaplysine | Homo sapiens (human) | IC50 | 250.0000 | 1 | 1 |
| 5-Chloro-1H-indole-2,3-dione | Homo sapiens (human) | IC50 | 1,000.0000 | 1 | 1 |
| o(6)-n-butylguanine | Homo sapiens (human) | IC50 | 42.6667 | 2 | 3 |
| cercosporamide | Homo sapiens (human) | IC50 | 0.7700 | 1 | 1 |
| birb 796 | Homo sapiens (human) | IC50 | 30.0000 | 1 | 1 |
| cyc 202 | Homo sapiens (human) | IC50 | 0.8752 | 17 | 21 |
| cyc 202 | Homo sapiens (human) | Ki | 0.2500 | 1 | 1 |
| sb 216763 | Homo sapiens (human) | IC50 | 0.2690 | 1 | 1 |
| 2,4-diamino-6-benzyloxy-5-nitrosopyrimidine | Homo sapiens (human) | IC50 | 27.0000 | 2 | 3 |
| paullone | Homo sapiens (human) | IC50 | 2.7000 | 1 | 1 |
| nu 6027 | Homo sapiens (human) | IC50 | 2.4000 | 5 | 7 |
| nu 6027 | Homo sapiens (human) | Ki | 1.9000 | 1 | 2 |
| 2H-pyrazolo[4,3-b]quinoxalin-3-amine | Homo sapiens (human) | IC50 | 0.0100 | 1 | 1 |
| 7-n-butyl-6-(4'-hydroxyphenyl)-5h-pyrrolo(2,3b)pyrazine | Homo sapiens (human) | IC50 | 0.1200 | 1 | 1 |
| 6-bromoindirubin-3'-oxime | Homo sapiens (human) | IC50 | 0.0690 | 1 | 1 |
| purvalanol b | Homo sapiens (human) | IC50 | 0.0060 | 2 | 2 |
| purvalanol a | Homo sapiens (human) | IC50 | 0.0556 | 5 | 7 |
| 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 | 0.0040 | 1 | 1 |
| cgp 74514a | Homo sapiens (human) | IC50 | 0.0460 | 1 | 1 |
| 1,4-dimethoxy-10H-acridine-9-thione | Homo sapiens (human) | IC50 | 20.0000 | 1 | 1 |
| bms 387032 | Homo sapiens (human) | IC50 | 0.0427 | 3 | 3 |
| sb 415286 | Homo sapiens (human) | IC50 | 0.3800 | 1 | 1 |
| alsterpaullone | Homo sapiens (human) | IC50 | 0.0150 | 1 | 1 |
| harmine | Homo sapiens (human) | IC50 | 25.0000 | 3 | 3 |
| wogonin | Homo sapiens (human) | IC50 | 1.4600 | 1 | 1 |
| ellagic acid | Homo sapiens (human) | IC50 | 3.3900 | 1 | 1 |
| alvocidib | Homo sapiens (human) | IC50 | 0.3441 | 9 | 10 |
| alvocidib | Homo sapiens (human) | Ki | 0.1900 | 1 | 1 |
| su 9516 | Homo sapiens (human) | IC50 | 0.0270 | 1 | 1 |
| casein kinase ii | Homo sapiens (human) | IC50 | 2.3800 | 1 | 1 |
| arcyriaflavin a | Homo sapiens (human) | IC50 | 0.1350 | 1 | 1 |
| pd 0183812 | Homo sapiens (human) | IC50 | 8.1182 | 2 | 5 |
| palbociclib | Homo sapiens (human) | IC50 | 4.9413 | 10 | 11 |
| palbociclib | Homo sapiens (human) | Ki | 5.0000 | 1 | 1 |
| jnj-7706621 | Homo sapiens (human) | IC50 | 31.6365 | 2 | 14 |
| cyc 116 | Homo sapiens (human) | IC50 | 0.7400 | 1 | 2 |
| cvt 313 | Homo sapiens (human) | IC50 | 0.2200 | 1 | 1 |
| leucettamine b | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| nu 6140 | Homo sapiens (human) | IC50 | 407.0000 | 1 | 1 |
| sotrastaurin | Homo sapiens (human) | IC50 | 2.3000 | 1 | 1 |
| meridianin a | Homo sapiens (human) | IC50 | 3.1000 | 1 | 1 |
| at 7519 | Homo sapiens (human) | IC50 | 0.0630 | 7 | 8 |
| at 7519 | Homo sapiens (human) | Ki | 0.0440 | 1 | 1 |
| 4-[2-(2-chloro-4-fluoroanilino)-5-methyl-4-pyrimidinyl]-N-[(1S)-1-(3-chlorophenyl)-2-hydroxyethyl]-1H-pyrrole-2-carboxamide | Homo sapiens (human) | Ki | 0.4472 | 1 | 4 |
| cgp 57380 | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| 5,7-dihydroxy-2-methyl-8-(4-(3-hydroxy-1-methyl)-piperidinyl)-4h-1-benzopyran-4-one | Homo sapiens (human) | IC50 | 7.3000 | 3 | 3 |
| mk-8776 | Homo sapiens (human) | IC50 | 0.1600 | 1 | 1 |
| pha 848125 | Homo sapiens (human) | IC50 | 0.2855 | 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 | 0.0130 | 2 | 2 |
| azd5438 | Homo sapiens (human) | IC50 | 0.0450 | 2 | 2 |
| p276-00 | Homo sapiens (human) | IC50 | 0.2240 | 1 | 1 |
| meriolin 3 | Homo sapiens (human) | IC50 | 0.0110 | 3 | 3 |
| cink4 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| defactinib | Homo sapiens (human) | IC50 | 0.3440 | 1 | 0 |
| entrectinib | Homo sapiens (human) | IC50 | 1.0000 | 1 | 1 |
| (R)-DRF053 | Homo sapiens (human) | IC50 | 0.2900 | 1 | 1 |
| nms p715 | Homo sapiens (human) | IC50 | 55.0000 | 2 | 2 |
| ribociclib | Homo sapiens (human) | IC50 | 48.0000 | 2 | 2 |
| pha 793887 | Homo sapiens (human) | IC50 | 0.0080 | 1 | 1 |
| tak-632 | Homo sapiens (human) | IC50 | 0.5800 | 1 | 1 |
| sb 1518 | Homo sapiens (human) | IC50 | 3.9000 | 1 | 1 |
| abemaciclib | Homo sapiens (human) | IC50 | 0.1036 | 4 | 4 |
| dinaciclib | Homo sapiens (human) | IC50 | 0.0020 | 2 | 2 |
| nms p937 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| nms-p118 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| on123300 | Homo sapiens (human) | IC50 | 0.1070 | 2 | 2 |
| THZ531 | Homo sapiens (human) | IC50 | 1.3000 | 1 | 1 |
| can 508 | Homo sapiens (human) | IC50 | 31.8688 | 3 | 8 |
| can 508 | Homo sapiens (human) | Ki | 69.0000 | 1 | 1 |
| ((5z)5-(1,3-benzodioxol-5-yl)methylene-2-phenylamino-3,5-dihydro-4h-imidazol-4-one) | Homo sapiens (human) | IC50 | 20.0000 | 2 | 2 |
| ro 3306 | Homo sapiens (human) | IC50 | 0.2530 | 1 | 1 |
| hymenialdisine | Homo sapiens (human) | IC50 | 0.0700 | 1 | 1 |
| debromohymenialdisine | Homo sapiens (human) | IC50 | 8.6661 | 1 | 7 |
| nms-e973 | Homo sapiens (human) | IC50 | 0.0100 | 1 | 1 |
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| nu6102 | Homo sapiens (human) | Kd | 1.3100 | 1 | 1 |
| cyc 202 | Homo sapiens (human) | EC50 | 0.1510 | 1 | 1 |
Drugs with Other Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| purvalanol b | Homo sapiens (human) | ID50 | 0.0060 | 1 | 1 |
| alvocidib | Homo sapiens (human) | ID50 | 0.1000 | 1 | 1 |
How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases?Journal of medicinal chemistry, , 10-25, Volume: 61, Issue:20, 2018
Discovery and in vitro evaluation of potent TrkA kinase inhibitors: oxindole and aza-oxindoles.Bioorganic & medicinal chemistry letters, , Feb-23, Volume: 14, Issue:4, 2004
From Structure Modification to Drug Launch: A Systematic Review of the Ongoing Development of Cyclin-Dependent Kinase Inhibitors for Multiple Cancer Therapy.Journal of medicinal chemistry, , 05-12, Volume: 65, Issue:9, 2022
Anticancer potential of indirubins in medicinal chemistry: Biological activity, structural modification, and structure-activity relationship.European journal of medicinal chemistry, , Nov-05, Volume: 223, 2021
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
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
Emerging and Re-Emerging Warheads for Targeted Covalent Inhibitors: Applications in Medicinal Chemistry and Chemical Biology.Journal of medicinal chemistry, , 06-27, Volume: 62, Issue:12, 2019
Cyclin-Dependent Kinase 2 Inhibitors in Cancer Therapy: An Update.Journal of medicinal chemistry, , 05-09, Volume: 62, Issue:9, 2019
Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase 1A (DYRK1A) Inhibitors as Potential Therapeutics.Journal of medicinal chemistry, , 11-21, Volume: 61, Issue:22, 2018
How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases?Journal of medicinal chemistry, , 10-25, Volume: 61, Issue:20, 2018
Dissecting the determinants of cyclin-dependent kinase 2 and cyclin-dependent kinase 4 inhibitor selectivity.Journal of medicinal chemistry, , Sep-07, Volume: 49, Issue:18, 2006
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
Structure-based design of 2-arylamino-4-cyclohexylmethyl-5-nitroso-6-aminopyrimidine inhibitors of cyclin-dependent kinases 1 and 2.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 13, Issue:18, 2003
Design, synthesis and biological study of novel pyrido[2,3-d]pyrimidine as anti-proliferative CDK2 inhibitors.European journal of medicinal chemistry, , Volume: 46, Issue:12, 2011
Design, synthesis, and biological evaluation of novel pyrimidine derivatives as CDK2 inhibitors.European journal of medicinal chemistry, , Volume: 45, Issue:3, 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
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 (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
From Structure Modification to Drug Launch: A Systematic Review of the Ongoing Development of Cyclin-Dependent Kinase Inhibitors for Multiple Cancer Therapy.Journal of medicinal chemistry, , 05-12, Volume: 65, Issue:9, 2022
Anticancer potential of indirubins in medicinal chemistry: Biological activity, structural modification, and structure-activity relationship.European journal of medicinal chemistry, , Nov-05, Volume: 223, 2021
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
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
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
Design, synthesis and biological evaluation of pyrazol-furan carboxamide analogues as novel Akt kinase inhibitors.European journal of medicinal chemistry, , Jul-19, Volume: 117, 2016
Synthesis and biological evaluation of 3-([1,2,4]triazolo[4,3-a]pyridin-3-yl)-4-(indol-3-yl)-maleimides as potent, selective GSK-3β inhibitors and neuroprotective agents.Bioorganic & medicinal chemistry, , Mar-01, Volume: 23, Issue:5, 2015
Design and synthesis of pyrimidine molecules endowed with thiazolidin-4-one as new anticancer agents.European journal of medicinal chemistry, , Aug-18, Volume: 83, 2014
Development of highly potent and selective diaminothiazole inhibitors of cyclin-dependent kinases.Journal of medicinal chemistry, , May-23, Volume: 56, Issue:10, 2013
Comparative structural and functional studies of 4-(thiazol-5-yl)-2-(phenylamino)pyrimidine-5-carbonitrile CDK9 inhibitors suggest the basis for isotype selectivity.Journal of medicinal chemistry, , Feb-14, Volume: 56, Issue:3, 2013
Structural basis for Chk1 inhibition by UCN-01.The Journal of biological chemistry, , Nov-29, Volume: 277, Issue:48, 2002
From Structure Modification to Drug Launch: A Systematic Review of the Ongoing Development of Cyclin-Dependent Kinase Inhibitors for Multiple Cancer Therapy.Journal of medicinal chemistry, , 05-12, Volume: 65, Issue:9, 2022
Mechanistic selectivity investigation and 2D-QSAR study of some new antiproliferative pyrazoles and pyrazolopyridines as potential CDK2 inhibitors.European journal of medicinal chemistry, , Jun-05, Volume: 218, 2021
Design, synthesis and biological evaluation of novel histone deacetylase1/2 (HDAC1/2) and cyclin-dependent Kinase2 (CDK2) dual inhibitors against malignant cancer.European journal of medicinal chemistry, , Jul-15, Volume: 198, 2020
Discovery of novel 9H-purin derivatives as dual inhibitors of HDAC1 and CDK2.Bioorganic & medicinal chemistry letters, , 08-15, Volume: 29, Issue:16, 2019
A β-glucuronidase-responsive albumin-binding prodrug for potential selective kinase inhibitor-based cancer chemotherapy.European journal of medicinal chemistry, , Oct-05, Volume: 158, 2018
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
Substituted 4-(thiazol-5-yl)-2-(phenylamino)pyrimidines are highly active CDK9 inhibitors: synthesis, X-ray crystal structures, structure-activity relationship, and anticancer activities.Journal of medicinal chemistry, , Feb-14, Volume: 56, Issue:3, 2013
Comparative structural and functional studies of 4-(thiazol-5-yl)-2-(phenylamino)pyrimidine-5-carbonitrile CDK9 inhibitors suggest the basis for isotype selectivity.Journal of medicinal chemistry, , Feb-14, Volume: 56, Issue:3, 2013
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 selective and potent cyclin-dependent kinase inhibitors.European journal of medicinal chemistry, , Volume: 56, 2012
Synthesis and biological evaluation of a selective N- and p/q-type calcium channel agonist.ACS medicinal chemistry letters, , Dec-13, Volume: 3, Issue:12, 2012
Design, synthesis and biological study of novel pyrido[2,3-d]pyrimidine as anti-proliferative CDK2 inhibitors.European journal of medicinal chemistry, , Volume: 46, Issue:12, 2011
Design, synthesis, and testing of an 6-O-linked series of benzimidazole based inhibitors of CDK5/p25.Bioorganic & medicinal chemistry, , Jan-01, Volume: 19, Issue:1, 2011
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
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
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
The selectivity of protein kinase inhibitors: a further update.The Biochemical journal, , Dec-15, Volume: 408, Issue:3, 2007
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 2 Inhibitors in Cancer Therapy: An Update.Journal of medicinal chemistry, , 05-09, Volume: 62, Issue:9, 2019
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
Structure-based design of 2-arylamino-4-cyclohexylmethyl-5-nitroso-6-aminopyrimidine inhibitors of cyclin-dependent kinases 1 and 2.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 13, Issue:18, 2003
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
Current progress and novel strategies that target CDK12 for drug discovery.European journal of medicinal chemistry, , Oct-05, Volume: 240, 2022
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
Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections.Journal of medicinal chemistry, , 01-27, Volume: 65, Issue:2, 2022
Current progress and novel strategies that target CDK12 for drug discovery.European journal of medicinal chemistry, , Oct-05, Volume: 240, 2022
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
The selectivity of protein kinase inhibitors: a further update.The Biochemical journal, , Dec-15, Volume: 408, Issue:3, 2007
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
Recent Developments in the Biology and Medicinal Chemistry of CDK9 Inhibitors: An Update.Journal of medicinal chemistry, , 11-25, Volume: 63, Issue:22, 2020
Synthesis and biological evaluation of novel 5,6-dihydropyrimido[4,5-f]quinazoline derivatives as potent CDK2 inhibitors.Bioorganic & medicinal chemistry letters, , 11-01, Volume: 28, Issue:20, 2018
Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy.Journal of medicinal chemistry, , 10-13, Volume: 59, Issue:19, 2016
N-(1H-Pyrazol-3-yl)quinazolin-4-amines as a novel class of casein kinase 1δ/ε inhibitors: Synthesis, biological evaluation and molecular modeling studies.Bioorganic & medicinal chemistry letters, , 06-15, Volume: 27, Issue:12, 2017
Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B.Journal of medicinal chemistry, , Nov-08, Volume: 55, Issue:21, 2012
Beta-carbolines as specific inhibitors of cyclin-dependent kinases.Bioorganic & medicinal chemistry letters, , Apr-08, Volume: 12, Issue:7, 2002
From Structure Modification to Drug Launch: A Systematic Review of the Ongoing Development of Cyclin-Dependent Kinase Inhibitors for Multiple Cancer Therapy.Journal of medicinal chemistry, , 05-12, Volume: 65, Issue:9, 2022
Identification of a new series of flavopiridol-like structures as kinase inhibitors with high cytotoxic potency.European journal of medicinal chemistry, , Aug-01, Volume: 199, 2020
A review on flavones targeting serine/threonine protein kinases for potential anticancer drugs.Bioorganic & medicinal chemistry, , 03-01, Volume: 27, Issue:5, 2019
Design of Novel 3-Pyrimidinylazaindole CDK2/9 Inhibitors with Potent In Vitro and In Vivo Antitumor Efficacy in a Triple-Negative Breast Cancer Model.Journal of medicinal chemistry, , 12-14, Volume: 60, Issue:23, 2017
Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy.Journal of medicinal chemistry, , 10-13, Volume: 59, Issue:19, 2016
Comparative structural and functional studies of 4-(thiazol-5-yl)-2-(phenylamino)pyrimidine-5-carbonitrile CDK9 inhibitors suggest the basis for isotype selectivity.Journal of medicinal chemistry, , Feb-14, Volume: 56, Issue:3, 2013
Design, synthesis, and antiproliferative and CDK2-cyclin a inhibitory activity of novel flavopiridol analogues.Bioorganic & medicinal chemistry, , Jan-15, Volume: 15, Issue:2, 2007
Structure-based design and synthesis of 2-benzylidene-benzofuran-3-ones as flavopiridol mimics.Journal of medicinal chemistry, , Apr-25, Volume: 45, Issue:9, 2002
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
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
[no title available]Journal of medicinal chemistry, , 03-26, Volume: 63, Issue:6, 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
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 a potent and selective inhibitor of cyclin-dependent kinase 4/6.Journal of medicinal chemistry, , Apr-07, Volume: 48, Issue:7, 2005
From Structure Modification to Drug Launch: A Systematic Review of the Ongoing Development of Cyclin-Dependent Kinase Inhibitors for Multiple Cancer Therapy.Journal of medicinal chemistry, , 05-12, Volume: 65, Issue:9, 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
Development of Second-Generation CDK2 Inhibitors for the Prevention of Cisplatin-Induced Hearing Loss.Journal of medicinal chemistry, , 09-13, Volume: 61, Issue:17, 2018
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
A review on flavones targeting serine/threonine protein kinases for potential anticancer drugs.Bioorganic & medicinal chemistry, , 03-01, Volume: 27, Issue:5, 2019
[no title available]Journal of medicinal chemistry, , 02-22, Volume: 61, Issue:4, 2018
A chromatography-free isolation of rohitukine from leaves of Dysoxylum binectariferum: Evaluation for in vitro cytotoxicity, Cdk inhibition and physicochemical properties.Bioorganic & medicinal chemistry letters, , 08-01, Volume: 26, Issue:15, 2016
Medulloblastoma drugs in development: Current leads, trials and drawbacks.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
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
From Structure Modification to Drug Launch: A Systematic Review of the Ongoing Development of Cyclin-Dependent Kinase Inhibitors for Multiple Cancer Therapy.Journal of medicinal chemistry, , 05-12, Volume: 65, Issue:9, 2022
Discovery of kinase spectrum selective macrocycle (16E)-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 (SB1317/TG02), a potent inhibitor of cyclin dependent kinases (CDKs), Janus kJournal of medicinal chemistry, , Jan-12, Volume: 55, Issue:1, 2012
Design of Novel 3-Pyrimidinylazaindole CDK2/9 Inhibitors with Potent In Vitro and In Vivo Antitumor Efficacy in a Triple-Negative Breast Cancer Model.Journal of medicinal chemistry, , 12-14, Volume: 60, Issue:23, 2017
Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy.Journal of medicinal chemistry, , 10-13, Volume: 59, Issue:19, 2016
Meriolins (3-(pyrimidin-4-yl)-7-azaindoles): synthesis, kinase inhibitory activity, cellular effects, and structure of a CDK2/cyclin A/meriolin complex.Journal of medicinal chemistry, , Feb-28, Volume: 51, Issue:4, 2008
Structure-based design of orally bioavailable 1H-pyrrolo[3,2-c]pyridine inhibitors of mitotic kinase monopolar spindle 1 (MPS1).Journal of medicinal chemistry, , Dec-27, Volume: 56, Issue:24, 2013
Synthesis and SAR of new pyrazolo[4,3-h]quinazoline-3-carboxamide derivatives as potent and selective MPS1 kinase inhibitors.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 21, Issue:15, 2011
Third-generation CDK inhibitors: A review on the synthesis and binding modes of Palbociclib, Ribociclib and Abemaciclib.European journal of medicinal chemistry, , Jun-15, Volume: 172, 2019
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 the macrocycle 11-(2-pyrrolidin-1-yl-ethoxy)-14,19-dioxa-5,7,26-triaza-tetracyclo[19.3.1.1(2,6).1(8,12)]heptacosa-1(25),2(26),3,5,8,10,12(27),16,21,23-decaene (SB1518), a potent Janus kinase 2/fms-like tyrosine kinase-3 (JAK2/FLT3) inhibitor Journal of medicinal chemistry, , Jul-14, Volume: 54, Issue:13, 2011
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]Journal of medicinal chemistry, , 03-26, Volume: 63, Issue:6, 2020
Discovery of 6-(2-(dimethylamino)ethyl)-N-(5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazole-6-yl)pyrimidin-2-yl)-5,6,7,8-tetrahydro-1,6-naphthyridin-2-amine as a highly potent cyclin-dependent kinase 4/6 inhibitor for treatment of cancer.European journal of medicinal chemistry, , Sep-15, Volume: 178, 2019
How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases?Journal of medicinal chemistry, , 10-25, Volume: 61, Issue:20, 2018
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
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
Discovery of novel CDK inhibitors via scaffold hopping from CAN508.Bioorganic & medicinal chemistry letters, , 05-01, Volume: 28, Issue:8, 2018
Comparative structural and functional studies of 4-(thiazol-5-yl)-2-(phenylamino)pyrimidine-5-carbonitrile CDK9 inhibitors suggest the basis for isotype selectivity.Journal of medicinal chemistry, , Feb-14, Volume: 56, Issue:3, 2013
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
Chemical synthesis and biological validation of immobilized protein kinase inhibitory Leucettines.European journal of medicinal chemistry, , Volume: 62, 2013
Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B.Journal of medicinal chemistry, , Nov-08, Volume: 55, Issue:21, 2012
Enables
This protein enables 4 target(s):
| Target | Category | Definition |
|---|
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| 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] |
| 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] |
| protein domain specific binding | molecular function | Binding to a specific domain of a protein. [GOC:go_curators] |
Located In
This protein is located in 6 target(s):
| Target | Category | Definition |
|---|
| female pronucleus | cellular component | The pronucleus originating from the ovum that is being fertilized. [GOC:hjd, ISBN:0198506732] |
| male pronucleus | cellular component | The pronucleus originating from the spermatozoa that was involved in fertilization. [GOC:hjd, ISBN:0198506732] |
| 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] |
| 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 |
|---|
| 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] |
| 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 3 target(s):
| Target | Category | Definition |
|---|
| cyclin A2-CDK1 complex | cellular component | A protein complex consisting of cyclin A2 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] |
| cyclin A2-CDK2 complex | cellular component | A protein complex consisting of cyclin A2 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] |
| cyclin-dependent protein kinase holoenzyme complex | cellular component | Cyclin-dependent protein kinases (CDKs) are enzyme complexes that contain a kinase catalytic subunit associated with a regulatory cyclin partner. [GOC:krc, PMID:11602261] |
Involved In
This protein is involved in 24 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] |
| 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] |
| regulation of DNA replication | biological process | Any process that modulates the frequency, rate or extent of DNA replication. [GOC:go_curators] |
| DNA-templated transcription | biological process | The synthesis of an RNA transcript from a DNA template. [GOC:jl, GOC:txnOH] |
| Ras protein signal transduction | biological process | An intracellular signaling cassette in which a small monomeric GTPase of the Ras subfamily relays a signal. [GOC:bf] |
| animal organ regeneration | biological process | The regrowth of a lost or destroyed animal organ. [GOC:mah] |
| response to glucagon | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a glucagon stimulus. [GOC:sl] |
| cellular response to platelet-derived growth factor stimulus | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a platelet-derived growth factor stimulus. [GOC:yaf] |
| post-translational protein modification | biological process | The process of covalently altering one or more amino acids in a protein after the protein has been completely translated and released from the ribosome. [GOC:jsg] |
| cellular response to leptin stimulus | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a leptin stimulus. Leptin is a hormone manufactured primarily in the adipocytes of white adipose tissue, and the level of circulating leptin is directly proportional to the total amount of fat in the body. It plays a key role in regulating energy intake and energy expenditure, including appetite and metabolism. [GOC:yaf] |
| cell cycle G1/S phase transition | biological process | The cell cycle process by which a cell in G1 phase commits to S phase. [GOC:mtg_cell_cycle] |
| positive regulation of DNA-templated transcription | biological process | Any process that activates or increases the frequency, rate or extent of cellular DNA-templated transcription. [GOC:go_curators, GOC:txnOH] |
| 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] |
| cellular response to cocaine | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a cocaine stimulus. Cocaine is a crystalline alkaloid obtained from the leaves of the coca plant. [GOC:mah] |
| cellular response to luteinizing hormone stimulus | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a luteinizing hormone stimulus. [GOC:mah] |
| cellular response to estradiol stimulus | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of stimulus by estradiol, a C18 steroid hormone hydroxylated at C3 and C17 that acts as a potent estrogen. [GOC:mah] |
| cellular response to hypoxia | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a stimulus indicating lowered oxygen tension. Hypoxia, defined as a decline in O2 levels below normoxic levels of 20.8 - 20.95%, results in metabolic adaptation at both the cellular and organismal level. [GOC:mah] |
| cellular response to nitric oxide | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a nitric oxide stimulus. [GOC:mah, GOC:yaf] |
| cochlea development | biological process | The progression of the cochlea over time from its formation to the mature structure. The cochlea is the snail-shaped portion of the inner ear that is responsible for the detection of sound. [GOC:dph, GOC:tb] |
| cellular response to insulin-like growth factor stimulus | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of an insulin-like growth factor stimulus. [PMID:20042609] |
| positive regulation of DNA biosynthetic process | biological process | Any process that activates or increases the frequency, rate or extent of DNA biosynthetic process. [GOC:obol] |
| 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] |