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

JAK1 (P23458) - Overview - Molecular Target Synopsis

Protein


JAK1, Tyrosine-protein kinase JAK1
Enzyme Classification 2.7.10.2
UniProt P23458

Also Known as JAK1_HUMAN, JAK1, JAK1A, JAK1B

Tyrosine kinase of the non-receptor type, involved in the IFN-alpha/beta/gamma signal pathway (PubMed:7615558). Kinase partner for the interleukin (IL)-2 receptor (PubMed:11909529) as well as interleukin (IL)-10 receptor (PubMed:12133952). Interacts with IL31RA (PubMed:15194700). Interacts with IFNAR2 (PubMed:7759950). Interacts with IFNGR1 (PubMed:7615558). Interacts with JAKMIP1 (PubMed:15277531). Interacts with SHB (PubMed:12200137). Interacts (via N-terminus) with IL2RB and IL10RA (via its cytoplasmic domain) (PubMed:12133952). Interacts with FER.

6ELR
HUMAN JAK1 KINASE DOMAIN IN COMPLEX WITH COMPOUND 7
RCSB/PDB
Inspect Structure
See all 3D Structures for JAK1

Isoforms / Transcripts (Protein Coding)


Protein Length Ensembl Gene Ensembl Transcript Ensembl Protein Uniprot Isoform
1154ENSG00000162434ENST00000342505ENSP00000343204P23458-1

Drugs


JAK1 is targeted by Approved Drugs Baricitinib, Ruxolitinib. (see details)
Baricitinib
Ruxolitinib

Sub-cellular localization


UniProt: JAK1 is active in the following subcellular-locations: endomembrane system.
GO terms: JAK1 is active in the following subcellular-locations: cytoplasm, cytoskeleton, cytosol, endosome, focal adhesion, membrane, nucleus.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project JAK1 has gain in 1 cell-lines, loss in 3 cell-lines and no signal in 1001 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: TK_10, ACHN, RXF_393

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: MHH-ES-1, Hs 746T, TC-71

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: NHLF, HSMM, BJ

(see details)

RNA Interference


JAK1 was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: NOS1, CAMA1. (see details)

3D Structures


For JAK1 there are:
29 structures (52 chains) solved
24 are solved in complex with at least one small molecule ligand
1 are solved with an approved drug

JAK1 is solved in complex with the approved drug(s):

MI1/TOFACITINIB (3EYG_A).

(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


JAK1 has been screened with 2766 compounds (3893 bioactivities), 1551 compounds have bioactivities that show binding affinity of <= 500nM (1885 bioactivities). (see details)