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cyclin dependent kinase 19

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Target not currently curated in GtoImmuPdb

Target id: 1972

Nomenclature: cyclin dependent kinase 19

Abbreviated Name: CDK19

Family: CDK8 subfamily

Contents:

Gene and Protein Information Click here for help
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 Click here for help
CDC2L6 | CDC2-related protein kinase 6 | CDK11
Database Links Click here for help
Alphafold Q9BWU1 (Hs), Q8BWD8 (Mm)
BRENDA 2.7.11.22
ChEMBL Target CHEMBL6002 (Hs)
Ensembl Gene ENSG00000155111 (Hs), ENSMUSG00000038481 (Mm), ENSRNOG00000000583 (Rn)
Entrez Gene 23097 (Hs), 78334 (Mm), 309804 (Rn)
Human Protein Atlas ENSG00000155111 (Hs)
KEGG Enzyme 2.7.11.22
KEGG Gene hsa:23097 (Hs), mmu:78334 (Mm), rno:309804 (Rn)
OMIM 614720 (Hs)
Pharos Q9BWU1 (Hs)
RefSeq Nucleotide NM_015076 (Hs), NM_001168304 (Mm), NM_001107634 (Rn)
RefSeq Protein NP_055891 (Hs), NP_001161776 (Mm), NP_001101104 (Rn)
UniProtKB Q9BWU1 (Hs), Q8BWD8 (Mm)
Wikipedia CDK19 (Hs)
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
CCT251545 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.6 pKd 2
⤷ pKd 8.6 (Kd 2.54x10-9 M) [2]
Description: CDK19/cyclin C.
cortistatin A Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.0 pKd 1
⤷ pKd 8.0 (Kd 1x10-8 M) [1]
linifanib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.9 pKd 2
⤷ pKd 7.9 (Kd 1.19x10-8 M) [2]
Description: CDK19/cyclin C.
ponatinib Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 7.9 pKd 2
⤷ pKd 7.9 (Kd 1.19x10-8 M) [2]
Description: CDK19/cyclin C.
sorafenib Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure 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] Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 8.3 pIC50 5
⤷ pIC50 8.3 (IC50 5.6x10-9 M) [5]
JH-VIII-49 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.1 pIC50 4
⤷ pIC50 8.1 (IC50 8x10-9 M) [4]
pexidartinib Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure 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 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: 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 Small molecule or natural product Hs Inhibitor Inhibition 8.8 pKd
alvocidib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.2 pKd
linifanib Small molecule or natural product Hs Inhibitor Inhibition 7.1 pKd
foretinib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.1 pKd
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.7 pKd
doramapimod Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.7 pKd
sorafenib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 6.6 pKd
PLX-4720 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.2 pKd
BMS-387032 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.0 pKd
A-674563 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 5.9 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »
Immuno Process Associations
Immuno Process:  Inflammation
Immuno Process:  Immune regulation

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 16/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetoimmunopharmacology.org/GRAC/ObjectDisplayForward?objectId=1972.