activin A receptor type 2A | Type II receptor serine/threonine kinases | IUPHAR/BPS Guide to PHARMACOLOGY

Top ▲

activin A receptor type 2A

Target not currently curated in GtoImmuPdb

Target id: 1791

Nomenclature: activin A receptor type 2A

Abbreviated Name: ActR2

Family: Type II receptor serine/threonine kinases

Annotation status:  image of an orange circle Annotated and awaiting review. Please contact us if you can help with reviewing.  » Email us

Quaternary Structure: Complexes
Bone morphogenetic protein receptors
Growth/differentiation factor receptors
Activin receptors
Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 1 513 2q22.2-q23.3 ACVR2A activin A receptor type 2A
Mouse 1 513 2 Acvr2a activin receptor IIA
Rat 1 512 3q12 Acvr2a activin A receptor type 2A
Previous and Unofficial Names
activin A receptor, type II | activin receptor IIA | ActRIIa | activin receptor 2A | ACVR2 | activin A receptor type IIA
Database Links
BRENDA
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of Activin receptor type-IIA (ACVR2A) kinase domain in complex with dorsomorphin
PDB Id:  3Q4T
Ligand:  dorsomorphin
Resolution:  1.96Å
Species:  Human
References: 
Enzyme Reaction
EC Number: 2.7.11.30
Natural/Endogenous Ligands
myostatin {Sp: Human}
Comments: Endogenous ligands may include growth/differentiation factor-6 [1].

Download all structure-activity data for this target as a CSV file

Antibodies
Key to terms and symbols Click column headers to sort
Antibody Sp. Action Value Parameter Reference
bimagrumab Hs Binding 9.4 pKd 2
pKd 9.4 (Kd 4.34x10-10 M) [2]
Description: Binding affinity of clone MOR08159
DiscoveRx KINOMEscan® screen
A screen of 72 inhibitors against 456 human kinases. Quantitative data were derived using DiscoveRx KINOMEscan® platform.
http://www.discoverx.com/services/drug-discovery-development-services/kinase-profiling/kinomescan
Reference: 3-4

Key to terms and symbols Click column headers to sort
Target used in screen: ACVR2A
Ligand Sp. Type Action Value Parameter
PD-173955 Hs Inhibitor Inhibition 8.0 pKd
PP-242 Hs Inhibitor Inhibition 7.7 pKd
dasatinib Hs Inhibitor Inhibition 6.7 pKd
KW-2449 Hs Inhibitor Inhibition 6.5 pKd
NVP-TAE684 Hs Inhibitor Inhibition 5.7 pKd
lestaurtinib Hs Inhibitor Inhibition 5.6 pKd
SB203580 Hs Inhibitor Inhibition <5.5 pKd
ruboxistaurin Hs Inhibitor Inhibition <5.5 pKd
erlotinib Hs Inhibitor Inhibition <5.5 pKd
GSK690693 Hs Inhibitor Inhibition <5.5 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »

References

Show »

1. Asai-Coakwell M, March L, Dai XH, Duval M, Lopez I, French CR, Famulski J, De Baere E, Francis PJ, Sundaresan P et al.. (2013) Contribution of growth differentiation factor 6-dependent cell survival to early-onset retinal dystrophies. Hum. Mol. Genet., 22 (7): 1432-42. [PMID:23307924]

2. Berger C, Herrmann T, Lu C, Sheppard K-A, Trifilieff E, Urlinger S. (2013) Compositions and methods for increasing muscle growth. Patent number: US8388968. Assignee: Novartis Ag. Priority date: 27/04/2009. Publication date: 05/03/2013.

3. Davis MI, Hunt JP, Herrgard S, Ciceri P, Wodicka LM, Pallares G, Hocker M, Treiber DK, Zarrinkar PP. (2011) Comprehensive analysis of kinase inhibitor selectivity. Nat. Biotechnol., 29 (11): 1046-51. [PMID:22037378]

4. Wodicka LM, Ciceri P, Davis MI, Hunt JP, Floyd M, Salerno S, Hua XH, Ford JM, Armstrong RC, Zarrinkar PP et al.. (2010) Activation state-dependent binding of small molecule kinase inhibitors: structural insights from biochemistry. Chem. Biol., 17 (11): 1241-9. [PMID:21095574]

How to cite this page

Type II receptor serine/threonine kinases: activin A receptor type 2A. Last modified on 30/03/2016. Accessed on 20/11/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1791.