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

MAP4K1 (Q92918) - Overview - Molecular Target Synopsis

Protein


MAP4K1, Mitogen-activated protein kinase kinase kinase kinase 1
Enzyme Classification 2.7.11.1
UniProt Q92918

Also Known as M4K1_HUMAN, MAP4K1, HPK1

Serine/threonine-protein kinase, which may play a role in the response to environmental stress. Appears to act upstream of the JUN N-terminal pathway. May play a role in hematopoietic lineage decisions and growth regulation. Able to autophosphorylate. Interacts with MAP3K1. Interacts with FBXW8.

6CQF
CRYSTAL STRUCTURE OF HPK1 IN COMPLEX AN INHIBITOR G1858
RCSB/PDB
Inspect Structure
See all 3D Structures for MAP4K1

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


GO terms: MAP4K1 is active in the following subcellular-locations: cytoplasm, intracellular, membrane.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project MAP4K1 has gain in 10 cell-lines, loss in 1 cell-lines and no signal in 994 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: CCRF_CEM, MOLT_4, OVCAR_3

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: OCI-LY-3, COR-L26, SU-DHL-5

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: GM12878, CD20-positive B cell, SK-N-SH

(see details)

RNA Interference


MAP4K1 was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: RES259, HCC1954. (see details)

3D Structures


For MAP4K1 there are:
3 structures (5 chains) solved
2 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


MAP4K1 has been screened with 132 compounds (172 bioactivities), 20 compounds have bioactivities that show binding affinity of <= 500nM (28 bioactivities). (see details)