cyclin dependent kinase 1 | CDK1 subfamily | IUPHAR/BPS Guide to PHARMACOLOGY

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cyclin dependent kinase 1

Target not currently curated in GtoImmuPdb

Target id: 1961

Nomenclature: cyclin dependent kinase 1

Abbreviated Name: CDK1

Family: CDK1 subfamily

Annotation status:  image of an orange circle Annotated and awaiting review. Please contact us if you can help with reviewing.  » Email us

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 297 10q21.2 CDK1 cyclin dependent kinase 1
Mouse - 297 10 B5.3 Cdk1 cyclin-dependent kinase 1
Rat - 297 20p11 Cdk1 cyclin-dependent kinase 1
Previous and Unofficial Names
CDC2 | CDC28A | cell division cycle 2 homolog A | p34 protein kinase | p34
Database Links
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
RefSeq Nucleotide
RefSeq Protein
Enzyme Reaction
EC Number:
EC Number:

Download all structure-activity data for this target as a CSV file

Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
R547 Hs Inhibition 8.7 pKi 6
pKi 8.7 (Ki 2x10-9 M) [6]
Description: Assayed using CDK1/cyclin B complex.
CDK inhibitor 4.35 Hs Inhibition 7.1 pKi 16
pKi 7.1 (Ki 9x10-8 M) [16]
Description: Inhibition of CDK1/cyclin B1 complex.
BMS-387032 Hs Inhibition 6.3 pKi 12
pKi 6.3 (Ki 4.8x10-7 M) [12]
alsterpaullone 2-cyanoethyl Hs Inhibition 9.6 pIC50 7
pIC50 9.6 (IC50 2.3x10-10 M) [7]
Description: CDK1 in association with cyclin B
Cdk1/2 inhibitor III Hs Inhibition 9.2 pIC50 22
pIC50 9.2 (IC50 6x10-10 M) [22]
Description: CDK1/cyclin B complex
RGB-286638 Hs Inhibition 8.7 pIC50 4
pIC50 8.7 (IC50 2x10-9 M) [4]
Description: in association with cyclin B1
dinaciclib Hs Inhibition 8.5 pIC50 24
pIC50 8.5 (IC50 3x10-9 M) [24]
BMS-265246 Hs Inhibition 8.2 pIC50 35
pIC50 8.2 (IC50 6x10-9 M) [35]
JNJ-7706621 Hs Inhibition 8.2 pIC50 22
pIC50 8.2 (IC50 6.4x10-9 M) [22]
Description: CDK1 in association with cyclin B
roniciclib Hs Inhibition 8.1 pIC50 23
pIC50 8.1 (IC50 7x10-9 M) [23]
Description: CDK1/cyclin B complex
TG02 Hs Inhibition 8.1 pIC50 9
pIC50 8.1 (IC50 9x10-9 M) [9]
AZD5438 Hs Inhibition 7.8 pIC50 3
pIC50 7.8 (IC50 1.6x10-8 M) [3]
Description: CDK1/cyclin B1 complex.
voruciclib Hs Inhibition 7.6 pIC50 29
pIC50 7.6 (IC50 2.5x10-8 M) [29]
Description: Inhibition of CDK1/cyclinB
compound 89S [PMID: 19115845] Hs Inhibition 7.5 pIC50 26
pIC50 7.5 (IC50 3x10-8 M) [26]
Description: CDK1/cyclin B complex
aminopurvalanol A Hs Inhibition 7.5 pIC50 7
pIC50 7.5 (IC50 3.3x10-8 M) [7]
Description: CDK1 in association with cyclin B
BS-194 Hs Inhibition 7.5 pIC50 11
pIC50 7.5 (IC50 3.3x10-8 M) [11]
alsterpaullone Hs Inhibition 7.5 pIC50 21
pIC50 7.5 (IC50 3.5x10-8 M) [21]
Description: CDK1 in association with cyclin B
(R)-CR8 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 Hs Inhibition 7.3 pIC50 17
pIC50 7.3 (IC50 4.7x10-8 M) [17]
Description: In vitro inhibition of human CDK1/cyclin B.
7-hydroxystaurosporine Hs Inhibition 7.3 pIC50 14
pIC50 7.3 (IC50 5x10-8 M) [14]
compound 9b [PMID: 18986805] Hs Inhibition 7.2 pIC50 15
pIC50 7.2 (IC50 6x10-8 M) [15]
(S)-CR8 Hs Inhibition 7.2 pIC50 2
pIC50 7.2 (IC50 6x10-8 M) [2]
Description: Inhibition of CDK1/cyclin E complex in vitro.
CGP74514A Hs Inhibition 6.8 – 7.6 pIC50 13,17
pIC50 7.6 (IC50 2.5x10-8 M) [13]
pIC50 6.8 (IC50 1.47x10-7 M) [17]
Description: In vitro inhibition of human CDK1/cyclin B.
kinase inhibitor 2 [PMID: 30199702] Hs Inhibition 7.2 pIC50 5
pIC50 7.2 (IC50 7x10-8 M) [5]
Description: CDK1/cyclin B
riviciclib Hs Inhibition 7.1 pIC50 18
pIC50 7.1 (IC50 7.9x10-8 M) [18]
Description: CDK1/cyclin B complex
SU9516 Hs Inhibition 6.8 – 7.4 pIC50 17,20
pIC50 7.4 (IC50 4x10-8 M) [20]
Description: CDK1/cyclin B complex used in assay
pIC50 6.8 (IC50 1.68x10-7 M) [17]
Description: In vitro inhibition of CDK1/cyclin B.
aloisine A Hs Inhibition 6.8 pIC50 27
pIC50 6.8 (IC50 1.5x10-7 M) [27]
Description: CDK1 in association with cyclin B
THAL-SNS-032 Hs Inhibition 6.8 pIC50 28
pIC50 6.8 (IC50 1.71x10-7 M) [28]
Description: Biochemical inhibition of CDK1/CycB.
AT-7519 Hs Inhibition 6.7 pIC50 34
pIC50 6.7 (IC50 2.1x10-7 M) [34]
GSK-3 inhibitor IX Hs Inhibition 6.5 pIC50 25,32
pIC50 6.5 (IC50 3.2x10-7 M) [25,32]
Description: CDK1/cyclin B complex
compound 52 [PMID: 9677190] Hs Inhibition 6.5 pIC50 10
pIC50 6.5 (IC50 3.4x10-7 M) [10]
Description: CDK1/cyclin B complex
kenpaullone Mgl Inhibition 6.4 pIC50 37
pIC50 6.4 (IC50 4x10-7 M) [37]
Description: CDK1/cyclin B complex
Cdk1/5 inhibitor Hs Inhibition 6.2 pIC50 7
pIC50 6.2 (IC50 6x10-7 M) [7]
Description: CDK1/cyclin B complex
bohemine Hs Inhibition 6.0 pIC50 36
pIC50 6.0 (IC50 1.1x10-6 M) [36]
Description: CDK1/cyclin B complexes purified from sf9 cells
milciclib Hs Inhibition 5.9 pIC50 17
pIC50 5.9 (IC50 1.2x10-6 M) [17]
Description: In vitro inhibition of CDK1/cyclin B.
ICEC0942 Hs Inhibition 5.7 pIC50 30
pIC50 5.7 (IC50 1.8x10-6 M) [30]
Description: In a biochemical assay.
1-azakenpaullone Hs Inhibition 5.7 pIC50 19
pIC50 5.7 (IC50 2x10-6 M) [19]
Description: CDK1/cyclin B complex in assay
Cdk4 inhibitor Hs Inhibition 5.7 pIC50 38
pIC50 5.7 (IC50 2.1x10-6 M) [38]
Description: CDK1/cyclin B complex
Cdk2 inhibitor III Hs Inhibition 5.4 pIC50 7
pIC50 5.4 (IC50 4.2x10-6 M) [7]
Description: CDK1/cyclin B complex
Cdk1 inhibitor Hs Inhibition 5.2 pIC50 7
pIC50 5.2 (IC50 5.8x10-6 M) [7]
Description: CDK1/cyclin B complex
Cdk2 inhibitor IV Hs Inhibition 5.2 pIC50 31
pIC50 5.2 (IC50 6.6x10-6 M) [31]
Description: CDK1/cyclin B complex used in assay
CHIR-99021 Hs Inhibition 5.1 pIC50 33
pIC50 5.1 (IC50 8.8x10-6 M) [33]
View species-specific inhibitor tables
EMD Millipore KinaseProfilerTM screen/Reaction Biology Kinase HotspotSM screen
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.

Reference: 1,8

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 Hs Inhibitor Inhibition -1.8 0.0 -1.0
Cdk/Crk inhibitor Hs Inhibitor Inhibition -1.2 3.0 0.0
JNJ-7706621 Hs Inhibitor Inhibition 5.7 1.0 0.0
PKR inhibitor Hs Inhibitor Inhibition 7.8 1.0 -1.0
JAK3 inhibitor VI Hs Inhibitor Inhibition 9.0 1.0 0.0
alsterpaullone 2-cyanoethyl Hs Inhibitor Inhibition 9.9 3.0 0.0
staurosporine Hs Inhibitor Inhibition 10.2 0.5 -0.5
CGP74514A Hs Inhibitor Inhibition 16.4 19.0 4.0
aminopurvalanol A Hs Inhibitor Inhibition 17.0 69.0 19.0
K-252a 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 Hs Inhibitor Inhibition -0.2
staurosporine Hs Inhibitor Inhibition 2.7
JAK3 inhibitor VI Hs Inhibitor Inhibition 6.8
PKR inhibitor Hs Inhibitor Inhibition 7.6
Cdk/Crk inhibitor Hs Inhibitor Inhibition 7.7
JNJ-7706621 Hs Inhibitor Inhibition 10.3
K-252a Hs Inhibitor Inhibition 19.8
alsterpaullone 2-cyanoethyl Hs Inhibitor Inhibition 24.8
aminopurvalanol A Hs Inhibitor Inhibition 25.9
purvalanol A 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


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17. 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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19. 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]

20. 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]

21. 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]

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23. 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]

24. 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]

25. 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]

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How to cite this page

CDK1 subfamily: cyclin dependent kinase 1. Last modified on 17/06/2020. Accessed on 04/07/2020. IUPHAR/BPS Guide to PHARMACOLOGY,