Page last updated: 2024-08-07 16:55:15
Cyclin-A1
A cyclin-A1 that is encoded in the genome of human. [PRO:CNA, UniProtKB:P78396]
Synonyms
Research
Bioassay Publications (50)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 21 (42.00) | 29.6817 |
| 2010's | 26 (52.00) | 24.3611 |
| 2020's | 3 (6.00) | 2.80 |
Compounds (46)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| gw8510 | Homo sapiens (human) | IC50 | 0.0100 | 1 | 1 |
| nsc 664704 | Homo sapiens (human) | IC50 | 0.7300 | 2 | 2 |
| nu2058 | Homo sapiens (human) | IC50 | 17.0000 | 2 | 2 |
| nu2058 | Homo sapiens (human) | Ki | 12.0000 | 1 | 1 |
| nu6102 | Homo sapiens (human) | IC50 | 0.0054 | 1 | 1 |
| o(6)-benzylguanine | Homo sapiens (human) | IC50 | 35.0000 | 1 | 1 |
| 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 | 1 | 1 |
| staurosporine | Homo sapiens (human) | IC50 | 0.0013 | 4 | 4 |
| staurosporine | Homo sapiens (human) | Ki | 0.0040 | 1 | 1 |
| o(6)-n-butylguanine | Homo sapiens (human) | IC50 | 48.0000 | 1 | 1 |
| birb 796 | Homo sapiens (human) | IC50 | 30.0000 | 1 | 1 |
| cyc 202 | Homo sapiens (human) | IC50 | 1.3611 | 9 | 9 |
| 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 | 1 | 1 |
| paullone | Homo sapiens (human) | IC50 | 2.7000 | 1 | 1 |
| nu 6027 | Homo sapiens (human) | IC50 | 2.2000 | 1 | 1 |
| 7-n-butyl-6-(4'-hydroxyphenyl)-5h-pyrrolo(2,3b)pyrazine | Homo sapiens (human) | IC50 | 0.1200 | 1 | 1 |
| purvalanol b | Homo sapiens (human) | IC50 | 0.0060 | 1 | 1 |
| purvalanol a | Homo sapiens (human) | IC50 | 0.0500 | 2 | 2 |
| bms 387032 | Homo sapiens (human) | IC50 | 0.0210 | 1 | 1 |
| sb 415286 | Homo sapiens (human) | IC50 | 0.3800 | 1 | 1 |
| harmine | Homo sapiens (human) | IC50 | 32.5000 | 2 | 2 |
| ellagic acid | Homo sapiens (human) | IC50 | 3.3900 | 1 | 1 |
| alvocidib | Homo sapiens (human) | IC50 | 0.7850 | 2 | 2 |
| alvocidib | Homo sapiens (human) | Ki | 0.1900 | 1 | 1 |
| casein kinase ii | Homo sapiens (human) | IC50 | 2.3800 | 1 | 1 |
| pd 0183812 | Homo sapiens (human) | IC50 | 0.2090 | 1 | 1 |
| palbociclib | Homo sapiens (human) | IC50 | 5.0000 | 1 | 1 |
| jnj-7706621 | Homo sapiens (human) | IC50 | 0.0020 | 1 | 1 |
| leucettamine b | Homo sapiens (human) | IC50 | 10.0000 | 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 | 0.0470 | 1 | 1 |
| cgp 57380 | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| mk-8776 | Homo sapiens (human) | IC50 | 0.1600 | 1 | 1 |
| 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 | 1 | 1 |
| meriolin 3 | Homo sapiens (human) | IC50 | 0.0110 | 1 | 1 |
| quizartinib | Homo sapiens (human) | IC50 | 20.0000 | 1 | 1 |
| defactinib | Homo sapiens (human) | IC50 | 0.3440 | 1 | 0 |
| nms p715 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| pha 793887 | Homo sapiens (human) | IC50 | 0.0080 | 1 | 1 |
| sb 1518 | Homo sapiens (human) | IC50 | 3.9000 | 1 | 1 |
| dinaciclib | Homo sapiens (human) | IC50 | 0.0030 | 1 | 1 |
| nms p937 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| can 508 | Homo sapiens (human) | IC50 | 69.0000 | 1 | 1 |
| 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 | 30.0000 | 1 | 1 |
| hymenialdisine | Homo sapiens (human) | IC50 | 0.0700 | 1 | 1 |
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| 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 |
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
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
Tetrahydroindazole inhibitors of CDK2/cyclin complexes.European journal of medicinal chemistry, , Mar-15, Volume: 214, 2021
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
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
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
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
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 a selective N- and p/q-type calcium channel agonist.ACS medicinal chemistry letters, , Dec-13, Volume: 3, Issue:12, 2012
Synthesis and biological evaluation of selective and potent cyclin-dependent kinase inhibitors.European journal of medicinal chemistry, , Volume: 56, 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
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
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
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
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
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
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
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
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
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
3Journal of medicinal chemistry, , 08-12, Volume: 64, Issue:15, 2021
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
3Journal of medicinal chemistry, , 08-12, Volume: 64, Issue:15, 2021
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
Enables
This protein enables 2 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] |
Located In
This protein is located in 3 target(s):
| Target | Category | Definition |
|---|
| 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] |
| microtubule cytoskeleton | cellular component | The part of the cytoskeleton (the internal framework of a cell) composed of microtubules and associated proteins. [GOC:jl, ISBN:0395825172] |
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] |
| 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] |
Part Of
This protein is part of 3 target(s):
| Target | Category | Definition |
|---|
| cyclin A1-CDK1 complex | cellular component | A protein complex consisting of cyclin A1 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 A1-CDK2 complex | cellular component | A protein complex consisting of cyclin A1 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 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] |
Involved In
This protein is involved in 5 target(s):
| Target | Category | Definition |
|---|
| male meiosis I | biological process | A cell cycle process comprising the steps by which a cell progresses through male meiosis I, the first meiotic division in the male germline. [GOC:dph, GOC:mah] |
| spermatogenesis | biological process | The developmental process by which male germ line stem cells self renew or give rise to successive cell types resulting in the development of a spermatozoa. [GOC:jid, ISBN:9780878933846, PMID:28073824, PMID:30990821] |
| 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] |
| 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] |