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cyclin dependent kinase 12

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Target not currently curated in GtoImmuPdb

Target id: 1965

Nomenclature: cyclin dependent kinase 12

Abbreviated Name: CDK12

Family: CRK7 subfamily

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 1490 17q12 CDK12 cyclin dependent kinase 12
Mouse - 1484 11 61.75 cM Cdk12 cyclin dependent kinase 12
Rat - 1484 10q31 Cdk12 cyclin-dependent kinase 12
Previous and Unofficial Names Click here for help
CDC2 related protein kinase 7 | cell division cycle 2-related protein kinase 7 | CRK7 | CRKR
Database Links Click here for help
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
RefSeq Nucleotide
RefSeq Protein
Enzyme Reaction Click here for help
EC Number:
EC Number:

Download all structure-activity data for this target as a CSV file go icon to follow link

Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
CDK12 inhibitor 2 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 7.3 pIC50 1
pIC50 7.3 (IC50 5.2x10-8 M) [1]
SY-5609 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 5.8 pIC50 2
pIC50 5.8 (IC50 1.702x10-6 M) [2]
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].


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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]

2. Marineau JJ, Hamman KB, Hu S, Alnemy S, Mihalich J, Kabro A, Whitmore KM, Winter DK, Roy S, Ciblat S et al.. (2022) Discovery of SY-5609: A Selective, Noncovalent Inhibitor of CDK7. J Med Chem, 65 (2): 1458-1480. [PMID:34726887]

How to cite this page

CRK7 subfamily: cyclin dependent kinase 12. Last modified on 12/01/2022. Accessed on 19/06/2024. IUPHAR/BPS Guide to PHARMACOLOGY,