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

NEK1 (Q96PY6) - Overview - Molecular Target Synopsis

Protein


NEK1, Serine/threonine-protein kinase Nek1
Enzyme Classification 2.7.11.1
UniProt Q96PY6

Also Known as NEK1_HUMAN, NEK1, KIAA1901

Phosphorylates serines and threonines, but also appears to possess tyrosine kinase activity (PubMed:20230784). Involved in DNA damage checkpoint control and for proper DNA damage repair (PubMed:20230784). In response to injury that includes DNA damage, NEK1 phosphorylates VDAC1 to limit mitochondrial cell death (PubMed:20230784). May be implicated in the control of meiosis (By similarity). Involved in cilium assembly (PubMed:21211617). Binds to SPERT (By similarity). Found in a complex with CFAP410, NEK1 and SPATA7 (PubMed:26167768). Interacts with CFAP410 (PubMed:26167768). Interacts (via Ser-1052 phosphorylated form) with 14-3-3 proteins.

4B9D
CRYSTAL STRUCTURE OF HUMAN NIMA-RELATED KINASE 1 (NEK1) WITH INHIBITOR.
RCSB/PDB
Inspect Structure
See all 3D Structures for NEK1

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


UniProt: NEK1 is active in the following subcellular-locations: centrosome, cytoplasm, cytoskeleton, microtubule organizing center, nucleus.
GO terms: NEK1 is active in the following subcellular-locations: centrosome, cytoplasm, nucleus, pericentriolar material.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project NEK1 has gain in 0 cell-lines, loss in 7 cell-lines and no signal in 998 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: A498, SNB_19, NCI_H460

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: MHH-NB-11, HCC193, OVCAR-8

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, A549, HSMM

(see details)

RNA Interference


NEK1 was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: DU4475, COV362. (see details)

3D Structures


For NEK1 there are:
2 structures (4 chains) solved
1 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


NEK1 has been screened with 622 compounds (1049 bioactivities), 96 compounds have bioactivities that show binding affinity of <= 500nM (99 bioactivities). (see details)