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

CDKL5 (O76039) - Overview - Molecular Target Synopsis

Protein


CDKL5, Cyclin-dependent kinase-like 5
Enzyme Classification 2.7.11.22
UniProt O76039

Also Known as CDKL5_HUMAN, CDKL5, STK9

Mediates phosphorylation of MECP2 (PubMed:15917271, PubMed:16935860). May regulate ciliogenesis (PubMed:29420175). Interacts with MECP2.

4BGQ
CRYSTAL STRUCTURE OF THE HUMAN CDKL5 KINASE DOMAIN
RCSB/PDB
Inspect Structure
See all 3D Structures for CDKL5

Isoforms / Transcripts (Protein Coding)


Protein Length Ensembl Gene Ensembl Transcript Ensembl Protein Uniprot Isoform
1030ENSG00000008086ENST00000379989, ENST00000379996ENSP00000369325, ENSP00000369332O76039-1
960O76039-2

Sub-cellular localization


UniProt: CDKL5 is active in the following subcellular-locations: centrosome, cilium basal body, cytoplasm, cytoskeleton, microtubule organizing center, nucleus.
GO terms: CDKL5 is active in the following subcellular-locations: centrosome, ciliary basal body, ciliary tip, cytosol, dendrite cytoplasm, dendritic growth cone, glutamatergic synapse, nucleoplasm, nucleus, perinuclear region of cytoplasm, postsynaptic density, ruffle membrane.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project CDKL5 has gain in 1 cell-lines, loss in 54 cell-lines and no signal in 950 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: RXF_393, OVCAR_4, EKVX

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: COLO-704, PLC/PRF/5, 786-O

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_RA, SK-N-SH, NHLF

(see details)

RNA Interference


CDKL5 was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: MDAMB157, MCF12A. (see details)

3D Structures


For CDKL5 there are:
1 structures (1 chains) solved
1 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


CDKL5 has been screened with 85 compounds (91 bioactivities), 7 compounds have bioactivities that show binding affinity of <= 500nM (8 bioactivities). (see details)