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cyclin dependent kinase 2

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Target id: 1973

Nomenclature: cyclin dependent kinase 2

Abbreviated Name: CDK2

Family: CDK1 subfamily

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 298 12q13.2 CDK2 cyclin dependent kinase 2
Mouse - 346 10 D3 Cdk2 cyclin dependent kinase 2
Rat - 298 7q11 Cdk2 cyclin dependent kinase 2
Previous and Unofficial Names Click here for help
cell division protein kinase 2
Database Links Click here for help
Alphafold P24941 (Hs), P97377 (Mm), Q63699 (Rn)
BRENDA 2.7.11.22
ChEMBL Target CHEMBL301 (Hs)
Ensembl Gene ENSG00000123374 (Hs), ENSMUSG00000025358 (Mm), ENSRNOG00000006469 (Rn)
Entrez Gene 1017 (Hs), 12566 (Mm), 362817 (Rn)
Human Protein Atlas ENSG00000123374 (Hs)
KEGG Enzyme 2.7.11.22
KEGG Gene hsa:1017 (Hs), mmu:12566 (Mm), rno:362817 (Rn)
OMIM 116953 (Hs)
Pharos P24941 (Hs)
RefSeq Nucleotide NM_001798 (Hs), NM_016756 (Mm), NM_199501 (Rn)
RefSeq Protein NP_001789 (Hs), NP_058036 (Mm), NP_955795 (Rn)
SynPHARM 79363 (in complex with dinaciclib)
80839 (in complex with milciclib)
85569 (in complex with RO3306)
85570 (in complex with RO3306)
80716 (in complex with roniciclib)
80557 (in complex with seliciclib)
80574 (in complex with SU9516)
85577 (in complex with SU9516)
85576 (in complex with SU9516)
UniProtKB P24941 (Hs), P97377 (Mm), Q63699 (Rn)
Wikipedia CDK2 (Hs)
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  APO STRUCTURE OF HUMAN CYCLIN-DEPENDENT KINASE 2
PDB Id:  1PW2
Resolution:  1.95Å
Species:  Human
References:  54
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of human CDK2 in complex with the inhibitor SU9516.
PDB Id:  3PY0
Ligand:  SU9516
Resolution:  1.75Å
Species:  Human
References:  6
Image of receptor 3D structure from RCSB PDB
Description:  X-ray structure of CDK2/cyclin A complex with the kinase inhibitor PHA-848125 (milciclib).
PDB Id:  2wih
Ligand:  milciclib
Resolution:  2.5Å
Species:  Human
References:  8
Image of receptor 3D structure from RCSB PDB
Description:  Discovery of (4-Pyrazolyl)-2-Aminopyrimidines as Potent and Selective Inhibitors of Cyclin-Dependent Kinase 2
PDB Id:  8UV0
Ligand:  compound 17 [PMID: 38325398]
Resolution:  1.55Å
Species:  Human
References:  25
Enzyme Reaction Click here for help
EC Number: 2.7.11.22

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 9.3 pKd 14
⤷ pKd 9.3 (Kd 5.3x10-10 M) [14]
AT-7519 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs - 7.5 pKd 14
⤷ pKd 7.5 (Kd 3x10-8 M) [14]
BMS-387032 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.2 pKd 14
⤷ pKd 7.2 (Kd 6.9x10-8 M) [14]
PF-06873600 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 9.9 pKi 5
⤷ pKi 9.9 (Ki 1.2x10-10 M) [5]
Description: Evaluated in a CDK2/Cyclin E1 mobility shift assay.
aloisine Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 9.3 pKi 3
⤷ pKi 9.3 (Ki 5.3x10-10 M) [3]
Description: Measuring inhibition of CDK2 in association with cyclin E
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 8.5 pKi 16
⤷ pKi 8.5 (Ki 3x10-9 M) [16]
Description: Assayed using CDK2/cyclin E complex.
asnuciclib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.5 pKi 44
⤷ pKi 8.5 (Ki 3x10-9 M) [44]
Description: Inhibition of human recombinant His6 tagged CDK2/Cyclin A expressed in Sf21 insect cells
BMS-387032 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.4 pKi 24
⤷ pKi 7.4 (Ki 3.8x10-8 M) [24]
seliciclib Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.6 pKi 24
⤷ pKi 6.6 (Ki 2.5x10-7 M) [24]
Description: CDK2/cyclin A complex used in assay
VTX-11e Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.1 pKi 4
⤷ pKi 6.1 (Ki 8.52x10-7 M) [4]
compound 17 [PMID: 38325398] Small molecule or natural product Ligand has a PDB structure Hs Inhibition 9.5 pIC50 25
⤷ pIC50 9.5 (IC50 2.9x10-10 M) [25]
QR-6401 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 9.4 pIC50 55
⤷ pIC50 9.4 (IC50 3.7x10-10 M) [55]
Description: Inhibition of CDK2/cyclin E1
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 9.3 pIC50 32
⤷ pIC50 9.3 (IC50 5x10-10 M) [32]
Description: CDK2/cyclin A complex
tanuxiciclib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 9.1 pIC50 11
⤷ pIC50 9.1 (IC50 9x10-10 M) [11]
Description: CDK2/cyclinE
compound 9b [PMID: 18986805] Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition >9.0 pIC50 26
⤷ pIC50 >9.0 (IC50 <1x10-9 M) [26]
tagtociclib Small molecule or natural product Hs Inhibition 8.9 pIC50 46
⤷ pIC50 8.9 (IC50 1.16x10-9 M) [46]
Description: Inhibition of CDK2/Cyclin E
dinaciclib Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 8.7 – 9.0 pIC50 27,35
⤷ pIC50 9.0 (IC50 1x10-9 M) [35]
pIC50 8.7 (IC50 2x10-9 M) [27]
Description: Inhibition of CDK2/cyclin E complex.
JNJ-7706621 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.7 pIC50 32
⤷ pIC50 8.7 (IC50 2x10-9 M) [32]
Description: CDK2 in association with cyclin A
compound 5g [PMID: 36385925] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.6 pIC50 47
⤷ pIC50 8.6 (IC50 2.6x10-9 M) [47]
RGB-286638 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 8.5 pIC50 12
⤷ pIC50 8.5 (IC50 3x10-9 M) [12]
Description: in association with cyclin E
BS-194 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.5 pIC50 23
⤷ pIC50 8.5 (IC50 3x10-9 M) [23]
CDK inhibitor 4.35 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.2 – 8.7 pIC50 27
⤷ pIC50 8.7 (IC50 2x10-9 M) [27]
Description: Inhibition of CDK2/cyclin E1 complex.
pIC50 8.2 (IC50 6x10-9 M) [27]
Description: Inhibition of CDK2/cyclin A2 complex.
compound 3 [PMID: 19097791] Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 8.4 pIC50 50
⤷ pIC50 8.4 (IC50 4.1x10-9 M) [50]
purvalanol B Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.2 pIC50 22
⤷ pIC50 8.2 (IC50 6x10-9 M) [22]
Description: CDK2/cyclin A complex used in assay
AZD5438 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.2 pIC50 9
⤷ pIC50 8.2 (IC50 6x10-9 M) [9]
Description: CDK2/cyclin E complex.
zotiraciclib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.9 – 8.3 pIC50 21,52
⤷ pIC50 7.9 – 8.3 (IC50 1.3x10-8 – 5x10-9 M) [21,52]
roniciclib Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 8.1 pIC50 34
⤷ pIC50 8.1 (IC50 9x10-9 M) [34]
Description: CDK2/cyclin E complex
BMS-265246 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 8.1 pIC50 49
⤷ pIC50 8.1 (IC50 9x10-9 M) [49]
AZD8421 Small molecule or natural product Hs Inhibition 7.2 – 8.1 pIC50 15
⤷ pIC50 8.1 (IC50 9x10-9 M) [15]
Description: Determined in a nanoBRET assay measuring cellular target engagement.
pIC50 7.2 (IC50 5.8x10-8 M) [15]
Description: Measuring inhibition of endogenous substrate phosphorylation in a cellular assay.
SU9516 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.6 – 7.7 pIC50 28,31
⤷ pIC50 7.7 (IC50 2.2x10-8 M) [31]
Description: CDK2/cyclin A complex used in assay
pIC50 7.6 (IC50 2.6x10-8 M) [28]
Description: In vitro inhibition of CDK2/cyclin E.
pIC50 7.6 (IC50 2.7x10-8 M) [28]
Description: In vitro inhibition of CDK2/cyclin A.
aminopurvalanol A Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 7.6 pIC50 17
⤷ pIC50 7.6 (IC50 2.8x10-8 M) [17]
Description: CDK2 in association with cyclin E
CGP74514A Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.3 – 7.6 pIC50 28
⤷ pIC50 7.6 (IC50 2.6x10-8 M) [28]
Description: In vitro inhibition of human CDK2/cyclin E.
pIC50 7.3 (IC50 4.6x10-8 M) [28]
Description: In vitro inhibition of human CDK2/cyclin A.
purvalanol A Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 7.5 pIC50 22
⤷ pIC50 7.5 (IC50 3.5x10-8 M) [22]
Description: CDK2/cyclin E complex used in assay
fadraciclib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.1 – 7.7 pIC50 45
⤷ pIC50 7.7 (IC50 2x10-8 M) [45]
Description: Inhibition of CDK2/cyclin E
pIC50 7.1 (IC50 9x10-8 M) [45]
Description: Inhibition of CDK2/cyclin A
AT-7519 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 48
⤷ pIC50 7.3 (IC50 4.7x10-8 M) [48]
THAL-SNS-032 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.2 pIC50 38
⤷ pIC50 7.2 (IC50 6.2x10-8 M) [38]
Description: Biochemical inhibition of CDK2/cyclin A
kinase inhibitor 2 [PMID: 30199702] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.2 pIC50 13
⤷ pIC50 7.2 (IC50 6.8x10-8 M) [13]
Description: CDK2/cyclin A
aloisine A Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 6.9 pIC50 37
⤷ pIC50 6.9 (IC50 1.2x10-7 M) [37]
Description: CDK2 in association with cyclin A
compound 89S [PMID: 19115845] Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.9 pIC50 36
⤷ pIC50 6.9 (IC50 1.38x10-7 M) [36]
Description: CDK2/cyclin A complex
MK-8776 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.8 pIC50 30
⤷ pIC50 6.8 (IC50 1.6x10-7 M) [30]
Description: CDK2/cyclin A complex in assay
milciclib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.2 – 7.3 pIC50 8,28
⤷ pIC50 7.3 (IC50 4.5x10-8 M) [8]
Description: CDK2/cyclin A complex
pIC50 7.0 (IC50 1.09x10-7 M) [28]
Description: In vitro inhibition of CDK2/cyclin A.
pIC50 6.2 (IC50 5.9x10-7 M) [28]
Description: In vitro inhibition of CDK2/cyclin E.
voruciclib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.7 pIC50 39
⤷ pIC50 6.7 (IC50 1.8x10-7 M) [39]
Description: Inhibition of CDK2/cyclinA
alvocidib Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.4 – 7.0 pIC50 10,33
⤷ pIC50 6.4 – 7.0 (IC50 4x10-7 – 1x10-7 M) [10,33]
Cdk4 inhibitor III Small molecule or natural product Click here for species-specific activity table Hs Inhibition <6.7 pIC50 42
⤷ pIC50 <6.7 (IC50 >2x10-7 M) [42]
Description: CDK2/cyclin A complex
RO3306 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.6 – 6.7 pIC50 28
⤷ pIC50 6.7 (IC50 1.86x10-7 M) [28]
Description: In vitro inhibition of human CDK2/cyclin E.
pIC50 6.6 (IC50 2.53x10-7 M) [28]
Description: In vitro inhibition of human CDK2/cyclin A.
istisociclib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.4 pIC50 19
⤷ pIC50 6.4 (IC50 3.97x10-7 M) [19]
Description: Inhibition of CDK2/Cyclin A
Cdk2 inhibitor IV Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.4 – 6.4 pIC50 28,41
⤷ pIC50 6.4 (IC50 4x10-7 M) [28]
pIC50 6.4 (IC50 4.1x10-7 M) [41]
Description: CDK2/cyclin A complex used in assay
BX-795 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 6.4 pIC50 18
⤷ pIC50 6.4 (IC50 4.3x10-7 M) [18]
Cdk2 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 6.3 pIC50 43
⤷ pIC50 6.3 (IC50 5x10-7 M) [43]
Description: CDK2/cyclin E complex
Cdk4 inhibitor Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.3 pIC50 57
⤷ pIC50 6.3 (IC50 5.2x10-7 M) [57]
Description: CDK2/cyclin E complex
bohemine Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 6.2 pIC50 51
⤷ pIC50 6.2 (IC50 6x10-7 M) [51]
Description: CDK2/cyclin E complexes purified from sf9 cells.
samuraciclib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.2 pIC50 40
⤷ pIC50 6.2 (IC50 6.2x10-7 M) [40]
Description: In a biochemical assay.
BX-912 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.2 pIC50 18
⤷ pIC50 6.2 (IC50 6.5x10-7 M) [18]
kenpaullone Small molecule or natural product Primary target of this compound Click here for species-specific activity table Mgl Inhibition 6.2 pIC50 56
⤷ pIC50 6.2 (IC50 6.8x10-7 M) [56]
Description: CDK2/cyclin A complex
BS-181 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.1 pIC50 1
⤷ pIC50 6.1 (IC50 8.8x10-7 M) [1]
Description: Evaluated using purified recombinant CDK2/cycE complex and measuring free ATP remaining in the reaction using a luciferase assay.
trilaciclib Small molecule or natural product Approved drug Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 5.9 pIC50 7
⤷ pIC50 5.9 (IC50 1.29x10-6 M) [7]
Description: Inhibition of CDK2/cyclinA
Cdk4 inhibitor II Small molecule or natural product Click here for species-specific activity table Hs Inhibition <4.0 pIC50 29
⤷ pIC50 <4.0 (IC50 >1x10-4 M) [29]
Description: CDK2/cyclin A complex used in assay
View species-specific inhibitor tables
DiscoveRx KINOMEscan® screen Click here for help
A screen of 72 inhibitors against 456 human kinases. Quantitative data were derived using DiscoveRx KINOMEscan® platform.
http://www.discoverx.com/services/drug-discovery-development-services/kinase-profiling/kinomescan
Reference: 14,53
Key to terms and symbols Click column headers to sort
Target used in screen: CDK2
Ligand Sp. Type Action Value Parameter
R547 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 9.3 pKd
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.1 pKd
lestaurtinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 7.7 pKd
AT-7519 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.5 pKd
BMS-387032 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.2 pKd
AST-487 Small molecule or natural product Hs Inhibitor Inhibition 6.3 pKd
alvocidib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.3 pKd
SB203580 Small molecule or natural product Immunopharmacology Ligand Hs Inhibitor Inhibition <5.5 pKd
ruboxistaurin Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition <5.5 pKd
erlotinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition <5.5 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »
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: 2,20
Key to terms and symbols Click column headers to sort
Target used in screen: CDK2-cyclin A/CDK2-cyclin A
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 0.3 -1.0 0.0
PKR inhibitor Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 0.9 1.0 0.0
Cdk1/2 inhibitor III Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 1.6 -2.0 -1.0
Cdk/Crk inhibitor Small molecule or natural product Hs Inhibitor Inhibition 2.0 0.0 0.0
JAK3 inhibitor VI Small molecule or natural product Hs Inhibitor Inhibition 2.1 1.0 0.0
JNJ-7706621 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 2.2 -1.0 1.0
alsterpaullone 2-cyanoethyl Small molecule or natural product Hs Inhibitor Inhibition 2.9 0.0 1.0
aminopurvalanol A Small molecule or natural product Hs Inhibitor Inhibition 4.1 34.0 4.0
K-252a Small molecule or natural product Hs Inhibitor Inhibition 4.2 1.0 0.0
purvalanol A Small molecule or natural product Hs Inhibitor Inhibition 6.9 3.0 0.0
Target used in screen: CDK2/cyclin E
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
PKR inhibitor Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 4.1
JNJ-7706621 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.1
aminopurvalanol A Small molecule or natural product Hs Inhibitor Inhibition 8.0
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.5
Cdk/Crk inhibitor Small molecule or natural product Hs Inhibitor Inhibition 8.6
Cdk1/2 inhibitor III Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.9
purvalanol A Small molecule or natural product Hs Inhibitor Inhibition 9.9
alsterpaullone 2-cyanoethyl Small molecule or natural product Hs Inhibitor Inhibition 13.4
JAK3 inhibitor VI Small molecule or natural product Hs Inhibitor Inhibition 14.5
GSK-3 inhibitor IX Small molecule or natural product Hs Inhibitor Inhibition 15.4
Target used in screen: CDK2/cyclinE
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 -1.0 -2.0
Cdk/Crk inhibitor Small molecule or natural product Hs Inhibitor Inhibition -1.0 -3.0
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 1.0 -0.5
alsterpaullone 2-cyanoethyl Small molecule or natural product Hs Inhibitor Inhibition 1.0 -2.0
PKR inhibitor Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 2.0 1.0
purvalanol A Small molecule or natural product Hs Inhibitor Inhibition 2.0 -1.0
JNJ-7706621 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 2.0 -1.0
GSK-3 inhibitor IX Small molecule or natural product Hs Inhibitor Inhibition 3.0 7.0
CGP74514A Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 4.0 -1.0
K-252a Small molecule or natural product Hs Inhibitor Inhibition 6.0 0.0
Displaying the top 10 most potent ligands  View all ligands in screen »

References

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2. 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]

3. Anderson PC, De Sapio V, Turner KB, Elmer SP, Roe DC, Schoeniger JS. (2012) Identification of binding specificity-determining features in protein families. J Med Chem, 55 (5): 1926-39. [PMID:22289061]

4. Aronov AM, Tang Q, Martinez-Botella G, Bemis GW, Cao J, Chen G, Ewing NP, Ford PJ, Germann UA, Green J et al.. (2009) Structure-guided design of potent and selective pyrimidylpyrrole inhibitors of extracellular signal-regulated kinase (ERK) using conformational control. J Med Chem, 52 (20): 6362-8. [PMID:19827834]

5. Behenna DC, Chen P, Freeman-Cook KD, Hoffman RL, Jalaie M, Nagata A, Nair SK, Ninkovic S, Ornelas MA, Palmer CL et al.. (2018) Pyridopyrimdinone cdk2/4/6 inhibitors. Patent number: WO2018033815A1. Assignee: Pfizer Inc.. Priority date: 15/08/2016. Publication date: 22/02/2018.

6. Betzi S, Alam R, Martin M, Lubbers DJ, Han H, Jakkaraj SR, Georg GI, Schönbrunn E. (2011) Discovery of a potential allosteric ligand binding site in CDK2. ACS Chem Biol, 6 (5): 492-501. [PMID:21291269]

7. Bisi JE, Sorrentino JA, Roberts PJ, Tavares FX, Strum JC. (2016) Preclinical Characterization of G1T28: A Novel CDK4/6 Inhibitor for Reduction of Chemotherapy-Induced Myelosuppression. Mol Cancer Ther, 15 (5): 783-93. [PMID:26826116]

8. Brasca MG, Amboldi N, Ballinari D, Cameron A, Casale E, Cervi G, Colombo M, Colotta F, Croci V, D'Alessio R et al.. (2009) 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. J Med Chem, 52 (16): 5152-63. [PMID:19603809]

9. 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]

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CDK1 subfamily: cyclin dependent kinase 2. Last modified on 23/05/2024. Accessed on 10/10/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=1973.