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

ACVR1 (Q04771) - Overview - Molecular Target Synopsis

Protein


ACVR1, Activin receptor type-1
Enzyme Classification 2.7.11.30
UniProt Q04771

Also Known as ACVR1_HUMAN, ACVR1, ACVRLK2

On ligand binding, forms a receptor complex consisting of two type II and two type I transmembrane serine/threonine kinases. Type II receptors phosphorylate and activate type I receptors which autophosphorylate, then bind and activate SMAD transcriptional regulators. Receptor for activin. May be involved for left-right pattern formation during embryogenesis. Interacts with FKBP1A. Interacts with FCHO1.

6ACR
CRYSTAL STRUCTURE OF HUMAN ALK2 KINASE DOMAIN WITH R206H MUTATION IN COMPLEX WITH RK-59638
RCSB/PDB
Inspect Structure
See all 3D Structures for ACVR1

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


UniProt: ACVR1 is active in the following subcellular-locations: membrane.
GO terms: ACVR1 is active in the following subcellular-locations: activin receptor complex, apical part of cell, integral component of plasma membrane, receptor complex.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project ACVR1 has gain in 2 cell-lines, loss in 2 cell-lines and no signal in 1001 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: HS578T, SF_539, MDA_N

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: Hs 746T, COLO-818, COLO 857

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, SK-N-SH

(see details)

RNA Interference


ACVR1 was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: MFM223, DU4475. (see details)

3D Structures


For ACVR1 there are:
14 structures (29 chains) solved
14 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


ACVR1 has been screened with 185 compounds (246 bioactivities), 43 compounds have bioactivities that show binding affinity of <= 500nM (56 bioactivities). (see details)