Tchem ACVR1 Activin receptor type-1

Protein Summary

Description

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 (By similarity). Activins are dimeric growth and differentiation factors which belong to the transforming growth factor-beta (TGF-beta) superfamily of structurally related signaling proteins. Activins signal through a heteromeric complex of receptor serine kinases which include at least two type I ( I and IB) and two type II (II and IIB) receptors. These receptors are all transmembrane proteins, composed of a ligand-binding extracellular domain with cysteine-rich region, a transmembrane domain, and a cytoplasmic domain with predicted serine/threonine specificity. Type I receptors are essential for signaling; and type II receptors are required for binding ligands and for expression of type I receptors. Type I and II receptors form a stable complex after ligand binding, resulting in phosphorylation of type I receptors by type II receptors. This gene encodes activin A type I receptor which signals a particular transcriptional response in concert with activin type II receptors. Mutations in this gene are associated with fibrodysplasia ossificans progressive. [provided by RefSeq, Jul 2008]

Uniprot Accession IDs

• Q04771

Gene Name

• ACVR1

Ensembl ID

• ENST00000263640
• ENSP00000263640
• ENSG00000115170
• ENST00000409283
• ENSP00000387273
• ENST00000410057
• ENSP00000387127
• ENST00000434821
• ENSP00000405004

Symbol

• ACVRLK2
• FOP
• ALK2
• SKR1
• TSRI
• ACTRI
• ACVR1A
• ACVRLK2

Knowledge Table

Most Knowledge About	Knowledge Value (0 to 1 scale)
molecular function	1
biological process	0.99
disease perturbation	0.97
protein domain	0.92
hub protein	0.79

Protein Classes

PANTHER Classes

Protein / Transferase / Kinase / Protein Kinase / Serine/threonine Protein Kinase Receptor / Activin Receptor Type-1

Protein / Receptor / Protein Kinase Receptor / Serine/threonine Protein Kinase Receptor / Activin Receptor Type-1

Protein / Receptor / Cytokine Receptor / Tgf-beta Receptor / Activin Receptor Type-1

DTO Classes

Protein / Kinase / Protein Kinase / Tkl Group / Stkr Family / Stkr Type 1 Subfamily / Activin Receptor Type-1

IDG Development Level Summary

Tdark

These are targets about which virtually nothing is known. They do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 401.42   (req: < 5)

Gene RIFs: 84   (req: <= 3)

Antibodies: 539   (req: <= 50)

Tbio

These targets do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 401.42   (req: >= 5)

Gene RIFs: 84   (req: > 3)

Antibodies: 539   (req: > 50)

- OR - satisfy the following criterion:

Gene Ontology Terms: 57

Tchem

Target has at least one ChEMBL compound with an activity cutoff of < 30 nM - AND - satisfies the preceding conditions

Active Ligands: 67

Tclin

Target has at least one approved drug - AND - satisfies the preceding conditions

Active Drug: 0

Protein Sequence and Structure

Residue Counts

Protein Sequence

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Expression Data (0 Tissues)

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No expression data found

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ProKinO

The ProKinO is a protein kinase-specific ontology, which provides a controlled vocabulary of terms, their hierarchy, and relationships unifying sequence, structure, function, mutation and pathway information on kinases.

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Target Illumination GWAS Analytics (TIGA)

TIGA scores and ranks GWAS discovered associations according to the quantity and quality of the evidence supporting the association.

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GENEVA

GENEVA (GENe Expression Variance Analysis) allows you to identify RNA-sequencing datasets from the Gene Expression Omnibus (GEO) that contain conditions modulating a gene or a gene signature.

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GlyGen

GlyGen is a data integration and dissemination project for carbohydrate and glycoconjugate related data.

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ARCHS4

ARCHS4 provides access to gene-function predictions based on RNA-seq co-expression, and gene expression levels across cell and tissues.

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Approved Drugs (0)

No approved drugs found

Active Ligands (67)

Explore Active Ligands

1 – 10 of 67

TAE-684

ACVR1Tchem Kinase

pKi : 8.5

PD166285

ACVR1Tchem Kinase

pKi : 8.1

XL-228

ACVR1Tchem Kinase

pKd : 7.58

PP-242

ACVR1Tchem Kinase

pKd : 8.32

saracatinib

ACVR1Tchem Kinase

pKd : 8

pacritinib

ACVR1Tchem Kinase

pKd : 7.28

momelotinib

ACVR1Tchem Kinase

pKd : 6.15

CHEMBL2385579

ACVR1Tchem Kinase

pIC50 : 8.86

CHEMBL2385582

ACVR1Tchem Kinase

pIC50 : 8.3

CHEMBL2385596

ACVR1Tchem Kinase

pIC50 : 8.3

Protein-Protein Interactions (115)

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1 – 10 of 115

• See Interactions on String-DB

LRRIQ1

Tdark

Novelty:  1.8251367

p_int:  0.999884701

p_ni:  0.000040716

p_wrong:  0.000074584

Score:  0.593

Data Source:  BioPlex,STRINGDB

TNFRSF10A

Tchem

Novelty:  0.0003383

p_int:  0.999864716

p_ni:  0.000077564

p_wrong:  0.00005772

Score:  0.663

Data Source:  BioPlex,STRINGDB

TGFBRAP1

Tbio

Novelty:  0.05996919

p_int:  0.963769973

p_ni:  0.03622065

p_wrong:  0.000009378

Score:  0.294

Data Source:  BioPlex,STRINGDB

BMPR1A

Tchem

Family:  Kinase

Novelty:  0.00343928

p_int:  0.949442782

p_ni:  0.050554372

p_wrong:  0.000002846

Score:  0.933

Data Source:  BioPlex,STRINGDB

BMPR2

Tchem

Family:  Kinase

Novelty:  0.00155912

p_int:  0.94729335

p_ni:  0.000047646

p_wrong:  0.052659005

Score:  0.991

Data Source:  BioPlex,STRINGDB

RNF149

Tdark

Family:  Enzyme

Novelty:  0.64503076

p_int:  0.93758666

p_ni:  0.062223718

p_wrong:  0.000189622

Score:  0.643

Data Source:  BioPlex,STRINGDB

MRAP2

Tbio

Novelty:  0.0420503

p_int:  0.93482703

p_ni:  0.000051895

p_wrong:  0.065121075

Score:  0.531

Data Source:  BioPlex,STRINGDB

GRAMD1A

Tbio

Novelty:  0.15461113

p_int:  0.898234711

p_ni:  0.101765286

p_wrong:  2e-9

Score:  0.152

Data Source:  BioPlex,STRINGDB

ACVRL1

Tchem

Family:  Kinase

Novelty:  0.00310167

p_int:  0.874917456

p_ni:  8e-9

p_wrong:  0.125082536

Score:  0.546

Data Source:  BioPlex,STRINGDB

CD320

Tbio

Novelty:  0.01978884

p_int:  0.857411228

p_ni:  0.142587369

p_wrong:  0.000001402

Score:  0.739

Data Source:  BioPlex,STRINGDB

Nearest Tclin Targets

Nearest Tclin calculations are only available for targets with KEGG Pathway annotations.

Pathways (192)

KEGG (4)

PathwayCommons (13)

WikiPathways (175)

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1 – 4 of 4

Data Source	Name	Explore in Pharos	Explore in Source
KEGG	TGF-beta signaling pathway	93 targets	path:hsa04350
KEGG	Signaling pathways regulating pluripotency of stem cells	139 targets	path:hsa04550
KEGG	Fluid shear stress and atherosclerosis	138 targets	path:hsa05418
KEGG	Cytokine-cytokine receptor interaction	290 targets	path:hsa04060

Name	Explore in Pharos	Explore in Source
TGF-beta signaling pathway	93 targets	path:hsa04350
Signaling pathways regulating pluripotency of stem cells	139 targets	path:hsa04550
Fluid shear stress and atherosclerosis	138 targets	path:hsa05418
Cytokine-cytokine receptor interaction	290 targets	path:hsa04060

Viral Interactions (0)

No viral interactions found

Gene Ontology Terms (61)

Functions (15)

Components (4)

Processes (42)

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10

1 – 10 of 15

GO Term	Evidence	Assigned by
activin binding	Inferred from Direct Assay (IDA)	UniProtKB
ATP binding	Inferred from Direct Assay (IDA)	HGNC
protein homodimerization activity	Inferred from Direct Assay (IDA)	BHF-UCL
protein kinase activity	Inferred from Direct Assay (IDA)	BHF-UCL
protein serine/threonine kinase activity	Inferred from Direct Assay (IDA)	HGNC
SMAD binding	Inferred from Direct Assay (IDA)	HGNC
transforming growth factor beta binding	Inferred from Direct Assay (IDA)	UniProtKB
BMP receptor activity	Inferred from Biological aspect of Ancestor (IBA)	GO_Central
growth factor binding	Inferred from Biological aspect of Ancestor (IBA)	GO_Central
transforming growth factor beta receptor activity, type I	Inferred from Biological aspect of Ancestor (IBA)	GO_Central

Disease Associations ()

No disease associations found

GWAS Traits (9)

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1 – 5 of 9

GWAS Trait	EFO ID	Study Count	SNP Count	Beta Count	Odds Ratio	Evidence (Mean Rank Score)	Provenance
BMI-adjusted waist-hip ratio	EFO_0007788	2	4	5		82.3
waist-hip ratio	EFO_0004343	1	4	4		61.3
waist circumference	EFO_0004342	1	4	4		60.2
reticulocyte count	EFO_0007986	2	2	2		55.1
BMI-adjusted waist circumference	EFO_0007789	1	4	4		50.6

• Explore on Target Illumination GWAS Analytics (TIGA)

Items per page:

5

1 – 5 of 9

GWAS Trait	EFO ID	Beta Count	Odds Ratio	Evidence (Mean Rank Score)	Provenance
BMI-adjusted waist-hip ratio	EFO_0007788	5		82.3
waist-hip ratio	EFO_0004343	4		61.3
waist circumference	EFO_0004342	4		60.2
reticulocyte count	EFO_0007986	2		55.1
BMI-adjusted waist circumference	EFO_0007789	4		50.6

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UniProt Keyword Find Similar Targets

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3D-structure
ATP-binding
Complete proteome
Disease mutation
Glycoprotein
Kinase
Magnesium
Manganese
Membrane
Metal-binding

GWAS Trait Find Similar Targets

No Header	No Header
BMI-adjusted waist circumference
BMI-adjusted waist-hip ratio
diastolic blood pressure
eosinophil count
eosinophil percentage of leukocytes
reticulocyte count
reticulocyte measurement
waist circumference
waist-hip ratio

MGI Phenotype Find Similar Targets

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behavior/neurological phenotype
cardiovascular system phenotype
cellular phenotype
craniofacial phenotype
digestive/alimentary phenotype
embryo phenotype
growth/size/body region phenotype
hearing/vestibular/ear phenotype
homeostasis/metabolism phenotype
immune system phenotype

IDG Resources

No IDG generated resources found

Orthologs (11)

1 – 5 of 11

Species	Name	Source ID	Gene ID	OMA	EggNOG	Inparanoid
Chimp	activin A receptor type 1	VGNC:56	470565
Macaque	activin A receptor type 1		697935
Mouse	activin A receptor, type 1	MGI:87911	11477
Rat	activin A receptor type 1	RGD:620200	79558
Dog	activin A receptor type 1	VGNC:37561	478757

Species	Name	OMA	EggNOG	Inparanoid
Chimp	activin A receptor type 1
Macaque	activin A receptor type 1
Mouse	activin A receptor, type 1
Rat	activin A receptor type 1
Dog	activin A receptor type 1

Publication Statistics

PubMed Score 401.42

PubMed score by year

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PubTator Score 213.98

PubTator score by year

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Patents

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Related Publications

Text Mined References (122)

GeneRif Annotations (84)

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PMID	Year	Title