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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

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
BRENDA
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Pharos
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
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 38
pIC50 8.2 (IC50 6x10-9 M) [38]
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.
QR-6401 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.7 pIC50 40
pIC50 7.7 (IC50 2.2x10-8 M) [40]
Description: Inhibition of CDK1/cyclin A2
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 Primary target of this compound 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 37
pIC50 6.7 (IC50 2.1x10-7 M) [37]
compound 5g [PMID: 36385925] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.5 pIC50 36
pIC50 6.5 (IC50 3.04x10-7 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 41
pIC50 6.4 (IC50 4x10-7 M) [41]
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 39
pIC50 6.0 (IC50 1.1x10-6 M) [39]
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 42
pIC50 5.7 (IC50 2.1x10-6 M) [42]
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 »

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]

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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]

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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]

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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]

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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]

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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]

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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. Sokolsky A, Winterton S, Kennedy K, Drake K, Stump K, Huo L, Lo Y, Ye M, Covington M, Diamond S et al.. (2022) Discovery of 5,7-Dihydro-6H-pyrrolo[2,3-d]pyrimidin-6-ones as Highly Selective CDK2 Inhibitors. ACS Med Chem Lett, 13 (11): 1797-1804. [PMID:36385925]

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CDK1 subfamily: cyclin dependent kinase 1. Last modified on 27/03/2023. Accessed on 04/12/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetoimmunopharmacology.org/GRAC/ObjectDisplayForward?objectId=1961.