Molecular Target Synopsis
Overview
Domains and Structures
Drugs and Clinical Candidates
Druggability
Chemistry
Ligand Efficiency Plot
Pathways
Family Cladogram
Interaction Network
Gene Expression
Gene Copy Number Variation
RNAi
Mutations
Germline Genetics

CLK1 (P49759) - Overview - Molecular Target Synopsis

Protein


CLK1, Dual specificity protein kinase CLK1
Enzyme Classification 2.7.12.1
UniProt P49759

Also Known as CLK1_HUMAN, CLK1, CLK

Dual specificity kinase acting on both serine/threonine and tyrosine-containing substrates. Phosphorylates serine- and arginine-rich (SR) proteins of the spliceosomal complex and may be a constituent of a network of regulatory mechanisms that enable SR proteins to control RNA splicing. Phosphorylates: SRSF1, SRSF3 and PTPN1. Regulates the alternative splicing of tissue factor (F3) pre-mRNA in endothelial cells and adenovirus E1A pre-mRNA. Interacts with PPIG and UBL5.

6Q8K
CLK1 WITH BOUND PYRIDOQUINAZOLINE
RCSB/PDB
Inspect Structure
See all 3D Structures for CLK1

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


UniProt: CLK1 is active in the following subcellular-locations: nucleus.
GO terms: CLK1 is active in the following subcellular-locations: cytoplasm, nucleus.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project CLK1 has gain in 0 cell-lines, loss in 1 cell-lines and no signal in 1004 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: RXF_393, HCT_15, HL_60

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: TYK-nu, HCC364, NCI-H596

In Array Express (RNA-seq of long poly adenylated RNA and long non poly adenylated RNA from ENCODE cell lines), the highest expressing cell lines are: SK-N-SH, NHLF, K562

(see details)

RNA Interference


CLK1 was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: H23, MCF12A. (see details)

3D Structures


For CLK1 there are:
15 structures (30 chains) solved
15 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


CLK1 has been screened with 682 compounds (784 bioactivities), 114 compounds have bioactivities that show binding affinity of <= 500nM (131 bioactivities). (see details)