cyclin dependent kinase 19 | CDK8 subfamily | IUPHAR/BPS Guide to PHARMACOLOGY

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cyclin dependent kinase 19

Target not currently curated in GtoImmuPdb

Target id: 1972

Nomenclature: cyclin dependent kinase 19

Abbreviated Name: CDK19

Family: CDK8 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 - 502 6q21 CDK19 cyclin dependent kinase 19
Mouse - 501 10 B1 Cdk19 cyclin-dependent kinase 19
Rat - 501 20q12 Cdk19 cyclin-dependent kinase 19
Previous and Unofficial Names
CDC2L6 | CDC2-related protein kinase 6 | CDK11
Database Links
BRENDA
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Pharos
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Enzyme Reaction
EC Number: 2.7.11.22

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

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
CCT251545 Hs Inhibition 8.6 pKd 2
pKd 8.6 (Kd 2.54x10-9 M) [2]
Description: CDK19/cyclin C.
cortistatin A Hs Inhibition 8.0 pKd 1
pKd 8.0 (Kd 1x10-8 M) [1]
linifanib Hs Inhibition 7.9 pKd 2
pKd 7.9 (Kd 1.19x10-8 M) [2]
Description: CDK19/cyclin C.
ponatinib Hs Inhibition 7.9 pKd 2
pKd 7.9 (Kd 1.19x10-8 M) [2]
Description: CDK19/cyclin C.
sorafenib Hs Inhibition 7.0 pKd 2
pKd 7.0 (Kd 1.03x10-7 M) [2]
Description: CDK19/cyclin C.
compound 51 [Mallinger et al., 2016] Hs Inhibition 8.3 pIC50 5
pIC50 8.3 (IC50 5.6x10-9 M) [5]
JH-VIII-49 Hs Inhibition 8.1 pIC50 4
pIC50 8.1 (IC50 8x10-9 M) [4]
pexidartinib Hs Inhibition 6.8 pIC50 6
pIC50 6.8 (IC50 1.4x10-7 M) [6]
Inhibitor Comments
The supplementary information from Cee et al. (2009) identifies the protein they refer to as CDK11 in the article text, as Entrez gene symbol CDC2L6 which is in fact CDK19, a close relation of CDK8 [1].
DiscoveRx KINOMEscan® screen
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: 3,7

Key to terms and symbols Click column headers to sort
Target used in screen: CDK11
Ligand Sp. Type Action Value Parameter
AST-487 Hs Inhibitor Inhibition 8.8 pKd
alvocidib Hs Inhibitor Inhibition 7.2 pKd
linifanib Hs Inhibitor Inhibition 7.1 pKd
foretinib Hs Inhibitor Inhibition 7.1 pKd
staurosporine Hs Inhibitor Inhibition 6.7 pKd
doramapimod Hs Inhibitor Inhibition 6.7 pKd
sorafenib Hs Inhibitor Inhibition 6.6 pKd
PLX-4720 Hs Inhibitor Inhibition 6.2 pKd
BMS-387032 Hs Inhibitor Inhibition 6.0 pKd
A-674563 Hs Inhibitor Inhibition 5.9 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »
Immuno Process Associations
Immuno Process:  Inflammation
GO Annotations:  Associated to 1 GO processes, IEA only
click arrow to show/hide IEA associations
GO:0050729 positive regulation of inflammatory response IEA
Immuno Process:  Immune regulation
GO Annotations:  Associated to 1 GO processes, IEA only
click arrow to show/hide IEA associations
GO:0050729 positive regulation of inflammatory response IEA

References

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1. Cee VJ, Chen DY, Lee MR, Nicolaou KC. (2009) Cortistatin A is a high-affinity ligand of protein kinases ROCK, CDK8, and CDK11. Angew. Chem. Int. Ed. Engl., 48 (47): 8952-7. [PMID:19844931]

2. Dale T, Clarke PA, Esdar C, Waalboer D, Adeniji-Popoola O, Ortiz-Ruiz MJ, Mallinger A, Samant RS, Czodrowski P, Musil D et al.. (2015) A selective chemical probe for exploring the role of CDK8 and CDK19 in human disease. Nat. Chem. Biol., 11 (12): 973-80. [PMID:26502155]

3. Davis MI, Hunt JP, Herrgard S, Ciceri P, Wodicka LM, Pallares G, Hocker M, Treiber DK, Zarrinkar PP. (2011) Comprehensive analysis of kinase inhibitor selectivity. Nat. Biotechnol., 29 (11): 1046-51. [PMID:22037378]

4. Hatcher JM, Wang ES, Johannessen L, Kwiatkowski N, Sim T, Gray NS. (2018) Development of Highly Potent and Selective Steroidal Inhibitors and Degraders of CDK8. ACS Med Chem Lett, 9 (6): 540-545. [PMID:29937979]

5. Mallinger A, Schiemann K, Rink C, Sejberg J, Honey MA, Czodrowski P, Stubbs M, Poeschke O, Busch M, Schneider R et al.. (2016) 2,8-Disubstituted-1,6-Naphthyridines and 4,6-Disubstituted-Isoquinolines with Potent, Selective Affinity for CDK8/19. ACS Med Chem Lett, 7 (6): 573-8. [PMID:27326329]

6. Tap WD, Wainberg ZA, Anthony SP, Ibrahim PN, Zhang C, Healey JH, Chmielowski B, Staddon AP, Cohn AL, Shapiro GI et al.. (2015) Structure-Guided Blockade of CSF1R Kinase in Tenosynovial Giant-Cell Tumor. N. Engl. J. Med., 373 (5): 428-37. [PMID:26222558]

7. Wodicka LM, Ciceri P, Davis MI, Hunt JP, Floyd M, Salerno S, Hua XH, Ford JM, Armstrong RC, Zarrinkar PP et al.. (2010) Activation state-dependent binding of small molecule kinase inhibitors: structural insights from biochemistry. Chem. Biol., 17 (11): 1241-9. [PMID:21095574]

How to cite this page

CDK8 subfamily: cyclin dependent kinase 19. Last modified on 05/04/2018. Accessed on 15/07/2020. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1972.