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cyclin dependent kinase 1

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Target not currently curated in GtoImmuPdb

Target id: 1961

Nomenclature: cyclin dependent kinase 1

Abbreviated Name: CDK1

Family: CDK1 subfamily

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 297 10q21.2 CDK1 cyclin dependent kinase 1
Mouse - 297 10 36.07 cM Cdk1 cyclin-dependent kinase 1
Rat - 297 20p11 Cdk1 cyclin-dependent kinase 1
Previous and Unofficial Names Click here for help
CDC2 | CDC28A | cell division cycle 2 homolog A | p34 protein kinase | p34
Database Links Click here for help
Alphafold P06493 (Hs), P11440 (Mm), P39951 (Rn)
BRENDA 2.7.11.22, 2.7.11.23
ChEMBL Target CHEMBL308 (Hs), CHEMBL4084 (Mm)
Ensembl Gene ENSG00000170312 (Hs), ENSMUSG00000019942 (Mm), ENSRNOG00000000632 (Rn)
Entrez Gene 983 (Hs), 12534 (Mm), 54237 (Rn)
Human Protein Atlas ENSG00000170312 (Hs)
KEGG Enzyme 2.7.11.22, 2.7.11.23
KEGG Gene hsa:983 (Hs), mmu:12534 (Mm), rno:54237 (Rn)
OMIM 116940 (Hs)
Pharos P06493 (Hs)
RefSeq Nucleotide NM_001170406 (Hs), NM_007659 (Mm), NM_019296 (Rn)
RefSeq Protein NP_031685 (Mm), NP_062169 (Rn)
UniProtKB P06493 (Hs), P11440 (Mm), P39951 (Rn)
Wikipedia CDK1 (Hs)
Enzyme Reaction Click here for help
EC Number: 2.7.11.22
EC Number: 2.7.11.23

Download all structure-activity data for this target as a CSV file go icon to follow link

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
R547 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.7 pKi 7
⤷ pKi 8.7 (Ki 2x10-9 M) [7]
Description: Assayed using CDK1/cyclin B complex.
asnuciclib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.4 pKi 35
⤷ pKi 8.4 (Ki 4x10-9 M) [35]
Description: Inhibition of human recombinant His6 tagged CDK1/Cyclin B expressed in Sf21 insect cells
CDK inhibitor 4.35 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.1 pKi 17
⤷ pKi 7.1 (Ki 9x10-8 M) [17]
Description: Inhibition of CDK1/cyclin B1 complex.
BMS-387032 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.3 pKi 13
⤷ pKi 6.3 (Ki 4.8x10-7 M) [13]
alsterpaullone 2-cyanoethyl Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 9.6 pIC50 8
⤷ pIC50 9.6 (IC50 2.3x10-10 M) [8]
Description: CDK1 in association with cyclin B
Cdk1/2 inhibitor III Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 9.2 pIC50 23
⤷ pIC50 9.2 (IC50 6x10-10 M) [23]
Description: CDK1/cyclin B complex
tanuxiciclib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 9.2 pIC50 4
⤷ pIC50 9.2 (IC50 6x10-10 M) [4]
Description: CDK1/cyclinD1
RGB-286638 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 8.7 pIC50 5
⤷ pIC50 8.7 (IC50 2x10-9 M) [5]
Description: in association with cyclin B1
dinaciclib Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 8.5 pIC50 25
⤷ pIC50 8.5 (IC50 3x10-9 M) [25]
BMS-265246 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 8.2 pIC50 37
⤷ pIC50 8.2 (IC50 6x10-9 M) [37]
JNJ-7706621 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.2 pIC50 23
⤷ pIC50 8.2 (IC50 6.4x10-9 M) [23]
Description: CDK1 in association with cyclin B
roniciclib Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 8.1 pIC50 24
⤷ pIC50 8.1 (IC50 7x10-9 M) [24]
Description: CDK1/cyclin B complex
zotiraciclib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.1 pIC50 10
⤷ pIC50 8.1 (IC50 9x10-9 M) [10]
AZD5438 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.8 pIC50 3
⤷ pIC50 7.8 (IC50 1.6x10-8 M) [3]
Description: CDK1/cyclin B1 complex.
voruciclib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.6 pIC50 30
⤷ pIC50 7.6 (IC50 2.5x10-8 M) [30]
Description: Inhibition of CDK1/cyclinB
compound 89S [PMID: 19115845] Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.5 pIC50 27
⤷ pIC50 7.5 (IC50 3x10-8 M) [27]
Description: CDK1/cyclin B complex
aminopurvalanol A Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 7.5 pIC50 8
⤷ pIC50 7.5 (IC50 3.3x10-8 M) [8]
Description: CDK1 in association with cyclin B
BS-194 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.5 pIC50 12
⤷ pIC50 7.5 (IC50 3.3x10-8 M) [12]
alsterpaullone Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.5 pIC50 22
⤷ pIC50 7.5 (IC50 3.5x10-8 M) [22]
Description: CDK1 in association with cyclin B
(R)-CR8 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.4 pIC50 2
⤷ pIC50 7.4 (IC50 4.1x10-8 M) [2]
Description: Inhibition of CDK1/cyclin E complex in vitro.
RO3306 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.3 pIC50 18
⤷ pIC50 7.3 (IC50 4.7x10-8 M) [18]
Description: In vitro inhibition of human CDK1/cyclin B.
7-hydroxystaurosporine Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.3 pIC50 15
⤷ pIC50 7.3 (IC50 5x10-8 M) [15]
compound 9b [PMID: 18986805] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.2 pIC50 16
⤷ pIC50 7.2 (IC50 6x10-8 M) [16]
(S)-CR8 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.2 pIC50 2
⤷ pIC50 7.2 (IC50 6x10-8 M) [2]
Description: Inhibition of CDK1/cyclin E complex in vitro.
CGP74514A Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.8 – 7.6 pIC50 14,18
⤷ pIC50 7.6 (IC50 2.5x10-8 M) [14]
pIC50 6.8 (IC50 1.47x10-7 M) [18]
Description: In vitro inhibition of human CDK1/cyclin B.
kinase inhibitor 2 [PMID: 30199702] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.2 pIC50 6
⤷ pIC50 7.2 (IC50 7x10-8 M) [6]
Description: CDK1/cyclin B
riviciclib Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 7.1 pIC50 19
⤷ pIC50 7.1 (IC50 7.9x10-8 M) [19]
Description: CDK1/cyclin B complex
SU9516 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.8 – 7.4 pIC50 18,21
⤷ pIC50 7.4 (IC50 4x10-8 M) [21]
Description: CDK1/cyclin B complex used in assay
pIC50 6.8 (IC50 1.68x10-7 M) [18]
Description: In vitro inhibition of CDK1/cyclin B.
aloisine A Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.8 pIC50 28
⤷ pIC50 6.8 (IC50 1.5x10-7 M) [28]
Description: CDK1 in association with cyclin B
THAL-SNS-032 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.8 pIC50 29
⤷ pIC50 6.8 (IC50 1.71x10-7 M) [29]
Description: Biochemical inhibition of CDK1/CycB.
AT-7519 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.7 pIC50 36
⤷ pIC50 6.7 (IC50 2.1x10-7 M) [36]
GSK-3 inhibitor IX Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.5 pIC50 26,33
⤷ pIC50 6.5 (IC50 3.2x10-7 M) [26,33]
Description: CDK1/cyclin B complex
compound 52 [PMID: 9677190] Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.5 pIC50 11
⤷ pIC50 6.5 (IC50 3.4x10-7 M) [11]
Description: CDK1/cyclin B complex
kenpaullone Small molecule or natural product Primary target of this compound Click here for species-specific activity table Mgl Inhibition 6.4 pIC50 39
⤷ pIC50 6.4 (IC50 4x10-7 M) [39]
Description: CDK1/cyclin B complex
Cdk1/5 inhibitor Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 6.2 pIC50 8
⤷ pIC50 6.2 (IC50 6x10-7 M) [8]
Description: CDK1/cyclin B complex
bohemine Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.0 pIC50 38
⤷ pIC50 6.0 (IC50 1.1x10-6 M) [38]
Description: CDK1/cyclin B complexes purified from sf9 cells
milciclib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 5.9 pIC50 18
⤷ pIC50 5.9 (IC50 1.2x10-6 M) [18]
Description: In vitro inhibition of CDK1/cyclin B.
samuraciclib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 5.7 pIC50 31
⤷ pIC50 5.7 (IC50 1.8x10-6 M) [31]
Description: In a biochemical assay.
1-azakenpaullone Small molecule or natural product Click here for species-specific activity table Hs Inhibition 5.7 pIC50 20
⤷ pIC50 5.7 (IC50 2x10-6 M) [20]
Description: CDK1/cyclin B complex in assay
Cdk4 inhibitor Small molecule or natural product Click here for species-specific activity table Hs Inhibition 5.7 pIC50 40
⤷ pIC50 5.7 (IC50 2.1x10-6 M) [40]
Description: CDK1/cyclin B complex
Cdk2 inhibitor III Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 5.4 pIC50 8
⤷ pIC50 5.4 (IC50 4.2x10-6 M) [8]
Description: CDK1/cyclin B complex
Cdk1 inhibitor Small molecule or natural product Primary target of this compound Hs Inhibition 5.2 pIC50 8
⤷ pIC50 5.2 (IC50 5.8x10-6 M) [8]
Description: CDK1/cyclin B complex
Cdk2 inhibitor IV Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 5.2 pIC50 32
⤷ pIC50 5.2 (IC50 6.6x10-6 M) [32]
Description: CDK1/cyclin B complex used in assay
laduviglusib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 5.1 pIC50 34
⤷ pIC50 5.1 (IC50 8.8x10-6 M) [34]
View species-specific inhibitor tables
EMD Millipore KinaseProfilerTM screen/Reaction Biology Kinase HotspotSM screen Click here for help
A screen profiling 158 kinase inhibitors (Calbiochem Protein Kinase Inhibitor Library I and II, catalogue numbers 539744 and 539745) for their inhibitory activity at 1µM and 10µM against 234 human recombinant kinases using the EMD Millipore KinaseProfilerTM service.

A screen profiling the inhibitory activity of 178 commercially available kinase inhibitors at 0.5µM against a panel of 300 recombinant protein kinases using the Reaction Biology Corporation Kinase HotspotSM platform.

http://www.millipore.com/techpublications/tech1/pf3036
http://www.reactionbiology.com/webapps/main/pages/kinase.aspx

Reference: 1,9
Key to terms and symbols Click column headers to sort
Target used in screen: CDK1-cyclin B/CDK1-cyclin B
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
Cdk1/2 inhibitor III Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition -1.8 0.0 -1.0
Cdk/Crk inhibitor Small molecule or natural product Hs Inhibitor Inhibition -1.2 3.0 0.0
JNJ-7706621 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 5.7 1.0 0.0
PKR inhibitor Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.8 1.0 -1.0
JAK3 inhibitor VI Small molecule or natural product Hs Inhibitor Inhibition 9.0 1.0 0.0
alsterpaullone 2-cyanoethyl Small molecule or natural product Hs Inhibitor Inhibition 9.9 3.0 0.0
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 10.2 0.5 -0.5
CGP74514A Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 16.4 19.0 4.0
aminopurvalanol A Small molecule or natural product Hs Inhibitor Inhibition 17.0 69.0 19.0
K-252a Small molecule or natural product Hs Inhibitor Inhibition 18.7 5.0 -1.0
Target used in screen: nd/CDK1-cyclin A
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
Cdk1/2 inhibitor III Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition -0.2
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 2.7
JAK3 inhibitor VI Small molecule or natural product Hs Inhibitor Inhibition 6.8
PKR inhibitor Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.6
Cdk/Crk inhibitor Small molecule or natural product Hs Inhibitor Inhibition 7.7
JNJ-7706621 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 10.3
K-252a Small molecule or natural product Hs Inhibitor Inhibition 19.8
alsterpaullone 2-cyanoethyl Small molecule or natural product Hs Inhibitor Inhibition 24.8
aminopurvalanol A Small molecule or natural product Hs Inhibitor Inhibition 25.9
purvalanol A Small molecule or natural product Hs Inhibitor Inhibition 31.7
Displaying the top 10 most potent ligands  View all ligands in screen »
Immuno Process Associations
Immuno Process:  Barrier integrity
GO Annotations:  Associated to 1 GO processes, IEA only
click arrow to show/hide IEA associations
GO:0001618 virus receptor activity IEA

References

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1. Anastassiadis T, Deacon SW, Devarajan K, Ma H, Peterson JR. (2011) Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity. Nat Biotechnol, 29 (11): 1039-45. [PMID:22037377]

2. Bettayeb K, Oumata N, Echalier A, Ferandin Y, Endicott JA, Galons H, Meijer L. (2008) CR8, a potent and selective, roscovitine-derived inhibitor of cyclin-dependent kinases. Oncogene, 27 (44): 5797-807. [PMID:18574471]

3. Byth KF, Thomas A, Hughes G, Forder C, McGregor A, Geh C, Oakes S, Green C, Walker M, Newcombe N et al.. (2009) AZD5438, a potent oral inhibitor of cyclin-dependent kinases 1, 2, and 9, leads to pharmacodynamic changes and potent antitumor effects in human tumor xenografts. Mol Cancer Ther, 8 (7): 1856-66. [PMID:19509270]

4. Changhee M, Oh B-g, Kim Y-e, Park C-m. (2016) Heterocyclic compound and pharmaceutical composition comprising same. Patent number: WO2016126085A2. Assignee: Beyond Bio. Priority date: 04/02/2015. Publication date: 03/11/2016.

5. Cirstea D, Hideshima T, Santo L, Eda H, Mishima Y, Nemani N, Hu Y, Mimura N, Cottini F, Gorgun G et al.. (2013) Small-molecule multi-targeted kinase inhibitor RGB-286638 triggers P53-dependent and -independent anti-multiple myeloma activity through inhibition of transcriptional CDKs. Leukemia, 27 (12): 2366-75. [PMID:23807770]

6. Compain G, Oumata N, Clarhaut J, Péraudeau E, Renoux B, Galons H, Papot S. (2018) A β-glucuronidase-responsive albumin-binding prodrug for potential selective kinase inhibitor-based cancer chemotherapy. Eur J Med Chem, 158: 1-6. [PMID:30199702]

7. DePinto W, Chu XJ, Yin X, Smith M, Packman K, Goelzer P, Lovey A, Chen Y, Qian H, Hamid R et al.. (2006) In vitro and in vivo activity of R547: a potent and selective cyclin-dependent kinase inhibitor currently in phase I clinical trials. Mol Cancer Ther, 5 (11): 2644-58. [PMID:17121911]

8. Fedorov O, Marsden B, Pogacic V, Rellos P, Müller S, Bullock AN, Schwaller J, Sundström M, Knapp S. (2007) A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. Proc Natl Acad Sci USA, 104 (51): 20523-8. [PMID:18077363]

9. Gao Y, Davies SP, Augustin M, Woodward A, Patel UA, Kovelman R, Harvey KJ. (2013) A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. Biochem J, 451 (2): 313-28. [PMID:23398362]

10. Goh KC, Novotny-Diermayr V, Hart S, Ong LC, Loh YK, Cheong A, Tan YC, Hu C, Jayaraman R, William AD et al.. (2012) TG02, a novel oral multi-kinase inhibitor of CDKs, JAK2 and FLT3 with potent anti-leukemic properties. Leukemia, 26 (2): 236-43. [PMID:21860433]

11. Gray NS, Wodicka L, Thunnissen AM, Norman TC, Kwon S, Espinoza FH, Morgan DO, Barnes G, LeClerc S, Meijer L et al.. (1998) Exploiting chemical libraries, structure, and genomics in the search for kinase inhibitors. Science, 281 (5376): 533-8. [PMID:9677190]

12. Heathcote DA, Patel H, Kroll SH, Hazel P, Periyasamy M, Alikian M, Kanneganti SK, Jogalekar AS, Scheiper B, Barbazanges M et al.. (2010) 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. J Med Chem, 53 (24): 8508-22. [PMID:21080703]

13. Hole AJ, Baumli S, Shao H, Shi S, Huang S, Pepper C, Fischer PM, Wang S, Endicott JA, Noble ME. (2013) Comparative structural and functional studies of 4-(thiazol-5-yl)-2-(phenylamino)pyrimidine-5-carbonitrile CDK9 inhibitors suggest the basis for isotype selectivity. J Med Chem, 56 (3): 660-70. [PMID:23252711]

14. Imbach P, Capraro HG, Furet P, Mett H, Meyer T, Zimmermann J. (1999) 2,6,9-trisubstituted purines: optimization towards highly potent and selective CDK1 inhibitors. Bioorg Med Chem Lett, 9 (1): 91-6. [PMID:9990463]

15. Jiang X, Zhao B, Britton R, Lim LY, Leong D, Sanghera JS, Zhou BB, Piers E, Andersen RJ, Roberge M. (2004) Inhibition of Chk1 by the G2 DNA damage checkpoint inhibitor isogranulatimide. Mol Cancer Ther, 3 (10): 1221-7. [PMID:15486189]

16. Jones CD, Andrews DM, Barker AJ, Blades K, Byth KF, Finlay MR, Geh C, Green CP, Johannsen M, Walker M et al.. (2008) Imidazole pyrimidine amides as potent, orally bioavailable cyclin-dependent kinase inhibitors. Bioorg Med Chem Lett, 18 (24): 6486-9. [PMID:18986805]

17. Jorda R, Havlíček L, Šturc A, Tušková D, Daumová L, Alam M, Škerlová J, Nekardová M, Peřina M, Pospíšil T et al.. (2019) 3,5,7-Substituted Pyrazolo[4,3- d]pyrimidine Inhibitors of Cyclin-Dependent Kinases and Their Evaluation in Lymphoma Models. J Med Chem, 62 (9): 4606-4623. DOI: 10.1021/acs.jmedchem.9b00189 [PMID:30943029]

18. Jorda R, Hendrychová D, Voller J, Řezníčková E, Gucký T, Kryštof V. (2018) How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases?. J Med Chem, 61 (20): 9105-9120. [PMID:30234987]

19. Joshi KS, Rathos MJ, Joshi RD, Sivakumar M, Mascarenhas M, Kamble S, Lal B, Sharma S. (2007) In vitro antitumor properties of a novel cyclin-dependent kinase inhibitor, P276-00. Mol Cancer Ther, 6 (3): 918-25. [PMID:17363486]

20. Kunick C, Lauenroth K, Leost M, Meijer L, Lemcke T. (2004) 1-Azakenpaullone is a selective inhibitor of glycogen synthase kinase-3 beta. Bioorg Med Chem Lett, 14 (2): 413-6. [PMID:14698171]

21. Lane ME, Yu B, Rice A, Lipson KE, Liang C, Sun L, Tang C, McMahon G, Pestell RG, Wadler S. (2001) A novel cdk2-selective inhibitor, SU9516, induces apoptosis in colon carcinoma cells. Cancer Res, 61 (16): 6170-7. [PMID:11507069]

22. Leost M, Schultz C, Link A, Wu YZ, Biernat J, Mandelkow EM, Bibb JA, Snyder GL, Greengard P, Zaharevitz DW et al.. (2000) Paullones are potent inhibitors of glycogen synthase kinase-3beta and cyclin-dependent kinase 5/p25. Eur J Biochem, 267 (19): 5983-94. [PMID:10998059]

23. Lin R, Connolly PJ, Huang S, Wetter SK, Lu Y, Murray WV, Emanuel SL, Gruninger RH, Fuentes-Pesquera AR, Rugg CA et al.. (2005) 1-Acyl-1H-[1,2,4]triazole-3,5-diamine analogues as novel and potent anticancer cyclin-dependent kinase inhibitors: synthesis and evaluation of biological activities. J Med Chem, 48 (13): 4208-11. [PMID:15974571]

24. Lücking U, Jautelat R, Krüger M, Brumby T, Lienau P, Schäfer M, Briem H, Schulze J, Hillisch A, Reichel A et al.. (2013) The lab oddity prevails: discovery of pan-CDK inhibitor (R)-S-cyclopropyl-S-(4-{[4-{[(1R,2R)-2-hydroxy-1-methylpropyl]oxy}-5-(trifluoromethyl)pyrimidin-2-yl]amino}phenyl)sulfoximide (BAY 1000394) for the treatment of cancer. ChemMedChem, 8 (7): 1067-85. [PMID:23671017]

25. Martin MP, Olesen SH, Georg GI, Schönbrunn E. (2013) Cyclin-dependent kinase inhibitor dinaciclib interacts with the acetyl-lysine recognition site of bromodomains. ACS Chem Biol, 8 (11): 2360-5. [PMID:24007471]

26. Meijer L, Skaltsounis AL, Magiatis P, Polychronopoulos P, Knockaert M, Leost M, Ryan XP, Vonica CA, Brivanlou A, Dajani R et al.. (2003) GSK-3-selective inhibitors derived from Tyrian purple indirubins. Chem Biol, 10 (12): 1255-66. [PMID:14700633]

27. Menichincheri M, Bargiotti A, Berthelsen J, Bertrand JA, Bossi R, Ciavolella A, Cirla A, Cristiani C, Croci V, D'Alessio R et al.. (2009) First Cdc7 kinase inhibitors: pyrrolopyridinones as potent and orally active antitumor agents. 2. Lead discovery. J Med Chem, 52 (2): 293-307. [PMID:19115845]

28. Mettey Y, Gompel M, Thomas V, Garnier M, Leost M, Ceballos-Picot I, Noble M, Endicott J, Vierfond JM, Meijer L. (2003) Aloisines, a new family of CDK/GSK-3 inhibitors. SAR study, crystal structure in complex with CDK2, enzyme selectivity, and cellular effects. J Med Chem, 46 (2): 222-36. [PMID:12519061]

29. Olson CM, Jiang B, Erb MA, Liang Y, Doctor ZM, Zhang Z, Zhang T, Kwiatkowski N, Boukhali M, Green JL et al.. (2018) Pharmacological perturbation of CDK9 using selective CDK9 inhibition or degradation. Nat Chem Biol, 14 (2): 163-170. [PMID:29251720]

30. Paiva C, Godbersen JC, Soderquist RS, Rowland T, Kilmarx S, Spurgeon SE, Brown JR, Srinivasa SP, Danilov AV. (2015) Cyclin-Dependent Kinase Inhibitor P1446A Induces Apoptosis in a JNK/p38 MAPK-Dependent Manner in Chronic Lymphocytic Leukemia B-Cells. PLoS ONE, 10 (11): e0143685. [PMID:26606677]

31. Patel H, Periyasamy M, Sava GP, Bondke A, Slafer BW, Kroll SHB, Barbazanges M, Starkey R, Ottaviani S, Harrod A et al.. (2018) ICEC0942, an Orally Bioavailable Selective Inhibitor of CDK7 for Cancer Treatment. Mol Cancer Ther, 17 (6): 1156-1166. [PMID:29545334]

32. Pennati M, Campbell AJ, Curto M, Binda M, Cheng Y, Wang LZ, Curtin N, Golding BT, Griffin RJ, Hardcastle IR et al.. (2005) Potentiation of paclitaxel-induced apoptosis by the novel cyclin-dependent kinase inhibitor NU6140: a possible role for survivin down-regulation. Mol Cancer Ther, 4 (9): 1328-37. [PMID:16170024]

33. Polychronopoulos P, Magiatis P, Skaltsounis AL, Myrianthopoulos V, Mikros E, Tarricone A, Musacchio A, Roe SM, Pearl L, Leost M et al.. (2004) Structural basis for the synthesis of indirubins as potent and selective inhibitors of glycogen synthase kinase-3 and cyclin-dependent kinases. J Med Chem, 47 (4): 935-46. [PMID:14761195]

34. Ring DB, Johnson KW, Henriksen EJ, Nuss JM, Goff D, Kinnick TR, Ma ST, Reeder JW, Samuels I, Slabiak T et al.. (2003) Selective glycogen synthase kinase 3 inhibitors potentiate insulin activation of glucose transport and utilization in vitro and in vivo. Diabetes, 52 (3): 588-95. [PMID:12606497]

35. Shao H, Shi S, Huang S, Hole AJ, Abbas AY, Baumli S, Liu X, Lam F, Foley DW, Fischer PM et al.. (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. J Med Chem, 56 (3): 640-59. [PMID:23301767]

36. Squires MS, Feltell RE, Wallis NG, Lewis EJ, Smith DM, Cross DM, Lyons JF, Thompson NT. (2009) Biological characterization of AT7519, a small-molecule inhibitor of cyclin-dependent kinases, in human tumor cell lines. Mol Cancer Ther, 8 (2): 324-32. [PMID:19174555]

37. Sutherland JJ, Low J, Blosser W, Dowless M, Engler TA, Stancato LF. (2011) A robust high-content imaging approach for probing the mechanism of action and phenotypic outcomes of cell-cycle modulators. Mol Cancer Ther, 10 (2): 242-54. [PMID:21216932]

38. Vermeulen K, Strnad M, Krystof V, Havlícek L, Van der Aa A, Lenjou M, Nijs G, Rodrigus I, Stockman B, van Onckelen H et al.. (2002) Antiproliferative effect of plant cytokinin analogues with an inhibitory activity on cyclin-dependent kinases. Leukemia, 16 (3): 299-305. [PMID:11896531]

39. Zaharevitz DW, Gussio R, Leost M, Senderowicz AM, Lahusen T, Kunick C, Meijer L, Sausville EA. (1999) Discovery and initial characterization of the paullones, a novel class of small-molecule inhibitors of cyclin-dependent kinases. Cancer Res, 59 (11): 2566-9. [PMID:10363974]

40. Zhu G, Conner SE, Zhou X, Shih C, Li T, Anderson BD, Brooks HB, Campbell RM, Considine E, Dempsey JA et al.. (2003) Synthesis, structure-activity relationship, and biological studies of indolocarbazoles as potent cyclin D1-CDK4 inhibitors. J Med Chem, 46 (11): 2027-30. [PMID:12747775]

How to cite this page

CDK1 subfamily: cyclin dependent kinase 1. Last modified on 29/07/2022. Accessed on 09/12/2022. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1961.