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

ACVRL1 (P37023) - Overview - Molecular Target Synopsis

Protein


ACVRL1, Serine/threonine-protein kinase receptor R3
Enzyme Classification 2.7.11.30
UniProt P37023

Also Known as ACVL1_HUMAN, ACVRL1, ACVRLK1, ALK1

Type I receptor for TGF-beta family ligands BMP9/GDF2 and BMP10 and important regulator of normal blood vessel development. 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. May bind activin as well.

2LCR
NMR STRUCTURE OF ALK1 EXTRACELLULAR DOMAIN
RCSB/PDB
Inspect Structure
See all 3D Structures for ACVRL1

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


UniProt: ACVRL1 is active in the following subcellular-locations: cell membrane.
GO terms: ACVRL1 is active in the following subcellular-locations: activin receptor complex, cell surface, dendrite, integral component of plasma membrane, neuronal cell body, plasma membrane, receptor complex.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project ACVRL1 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: TK_10, HL_60, SN12C

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: SK-N-DZ, SK-N-FI, Hs 895.T

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: HUVEC, hMSC-AT, HFDPC

(see details)

RNA Interference


ACVRL1 was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: SUM44, CAL120. (see details)

3D Structures


For ACVRL1 there are:
3 structures (34 chains) solved
1 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


ACVRL1 has been screened with 207 compounds (268 bioactivities), 78 compounds have bioactivities that show binding affinity of <= 500nM (91 bioactivities). (see details)