cyclin dependent kinase 12 | CRK7 subfamily | IUPHAR/BPS Guide to PHARMACOLOGY

Top ▲

cyclin dependent kinase 12

Target not currently curated in GtoImmuPdb

Target id: 1965

Nomenclature: cyclin dependent kinase 12

Abbreviated Name: CDK12

Family: CRK7 subfamily

Annotation status:  image of a grey circle Awaiting annotation/under development. Please contact us if you can help with annotation.  » Email us

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 1490 17q12 CDK12 cyclin dependent kinase 12
Mouse - 1484 11 D Cdk12 cyclin-dependent kinase 12
Rat - 1484 10q31 Cdk12 cyclin-dependent kinase 12
Previous and Unofficial Names
CDC2 related protein kinase 7 | cell division cycle 2-related protein kinase 7 | CRK7 | CRKR
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
EC Number: 2.7.11.23

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
CDK12 inhibitor 2 Hs Inhibition 7.3 pIC50 1
pIC50 7.3 (IC50 5.2x10-8 M) [1]
General Comments
Mutations in CDK12 that have been found in tumours and pharmacological CDK12 inhibition sensitise cancer cells to DNA-damaging reagents and DNA-repair inhibitors. This selective CDK12 inhibitors are being investigated for potential oncology efficacy. CDK12 inhibitor 2 is a compound that is a suitable tool for studying the effects of CDK12 inhibition in RNA biology and the role of this mechanism in inducing cancer cell synthetic lethality. CDK12 inhibitor 2 selectively inhibits CDK12 and the closely related CDK13 over other C-terminal domain serine kinases [1].

References

Show »

1. Ito M, Tanaka T, Toita A, Uchiyama N, Kokubo H, Morishita N, Klein MG, Zou H, Murakami M, Kondo M et al.. (2018) Discovery of 3-Benzyl-1-( trans-4-((5-cyanopyridin-2-yl)amino)cyclohexyl)-1-arylurea Derivatives as Novel and Selective Cyclin-Dependent Kinase 12 (CDK12) Inhibitors. J. Med. Chem., 61 (17): 7710-7728. [PMID:30067358]

How to cite this page

CRK7 subfamily: cyclin dependent kinase 12. Last modified on 28/08/2018. Accessed on 12/08/2020. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1965.