Molecular Target Synopsis
Domains and Structures
Drugs and Clinical Candidates
Ligand Efficiency Plot
Family Cladogram
Interaction Network
Gene Expression
Gene Copy Number Variation
Germline Genetics

GRK3 (P35626) - Overview - Molecular Target Synopsis


GRK3, Beta-adrenergic receptor kinase 2
Enzyme Classification
UniProt P35626

Also Known as ARBK2_HUMAN, GRK3, ADRBK2, BARK2

Specifically phosphorylates the agonist-occupied form of the beta-adrenergic and closely related receptors.

Isoforms / Transcripts (Protein Coding)

Protein Length Ensembl Gene Ensembl Transcript Ensembl Protein Uniprot Isoform

Sub-cellular localization

GO terms: GRK3 is active in the following subcellular-locations: cytosol, plasma membrane.

GO terms

Gene Copy Number Variation

In COSMIC - Cell Lines Project GRK3 has gain in 2 cell-lines, loss in 1 cell-lines and no signal in 1002 cell-lines. (see details)

Gene Expression

In NCI60, the highest expressing cell lines are:

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

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:

(see details)

RNA Interference

GRK3 was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: CROE33, H2228. (see details)

3D Structures

At greater than 75% identity similarity to GRK3 there are:
28 structures (31 chains) solved
20 are solved in complex with at least one small molecule ligand
1 are solved with an approved drug

GRK3 is solved in complex with the approved drug(s):


(see details)
Molecular Target 3D Synopsis

Screening and Chemistry

GRK3 has been screened with 53 compounds (60 bioactivities), 18 compounds have bioactivities that show binding affinity of <= 500nM (18 bioactivities). (see details)