Tchem ACVR1 Activin receptor type-1

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

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

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: 317.67   (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: 317.67   (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: 19

Tclin

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

Active Drug: 0

Active Ligands (19)

Explore Active Ligands

1 – 10 of 19

CHEMBL509032

ACVR1Tchem Kinase

Kd: 7.54

CHEMBL1241674

ACVR1Tchem Kinase

Kd: 8.4

CHEMBL2385579

ACVR1Tchem Kinase

IC50: 7.26999998

CHEMBL1078178

ACVR1Tchem Kinase

Kd: 7.6

CHEMBL2385582

ACVR1Tchem Kinase

IC50: 8.30000019

CHEMBL3341789

ACVR1Tchem Kinase

IC50: 7.62

CHEMBL2385596

ACVR1Tchem Kinase

IC50: 8.30000019

CHEMBL3818173

ACVR1Tchem Kinase

IC50: 8.92

CHEMBL3586447

ACVR1Tchem Kinase

IC50: 8.15

ML347

ACVR1Tchem Kinase

IC50: 7.48999977

Protein Data Bank (13)

1 – 5 of 13

PDB Structure Id	Ligand	Method	Resolution (Å)	M.W. (kDa)	Pub Year	Title

PDB Structure Id	M.W.	Resolution	Pub Year

Pathways (192)

KEGG (4)

PathwayCommons (13)

WikiPathways (175)

Items per page:

5

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

Gene Ontology Terms (61)

Functions (15)

Components (4)

Processes (42)

Items per page:

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

Protein-Protein Interactions (115)

Explore Interacting Targets

1 – 10 of 115

• See Interactions on String-DB

LRRIQ1

Tdark

p_int: 0.999884701

p_ni: 0.000040716

p_wrong: 0.000074584

Score: 0.593

Data Source: BioPlex,STRINGDB

TNFRSF10A

Tchem

Novelty: 0.0003938

p_int: 0.999864716

p_ni: 0.000077564

p_wrong: 0.00005772

Score: 0.663

Data Source: BioPlex,STRINGDB

TGFBRAP1

Tbio

Novelty: 0.09004245

p_int: 0.963769973

p_ni: 0.03622065

p_wrong: 0.000009378

Score: 0.294

Data Source: BioPlex,STRINGDB

BMPR1A

Tchem

Family: Kinase

Novelty: 0.00472897

p_int: 0.949442782

p_ni: 0.050554372

p_wrong: 0.000002846

Score: 0.933

Data Source: BioPlex,STRINGDB

BMPR2

Tchem

Family: Kinase

Novelty: 0.00191079

p_int: 0.94729335

p_ni: 0.000047646

p_wrong: 0.052659005

Score: 0.991

Data Source: BioPlex,STRINGDB

RNF149

Tdark

Family: Enzyme

Novelty: 0.47955733

p_int: 0.93758666

p_ni: 0.062223718

p_wrong: 0.000189622

Score: 0.643

Data Source: BioPlex,STRINGDB

MRAP2

Tbio

Novelty: 0.05863056

p_int: 0.93482703

p_ni: 0.000051895

p_wrong: 0.065121075

Score: 0.531

Data Source: BioPlex,STRINGDB

GRAMD1A

Tdark

Novelty: 0.3099631

p_int: 0.898234711

p_ni: 0.101765286

p_wrong: 2e-9

Score: 0.152

Data Source: BioPlex,STRINGDB

ACVRL1

Tchem

Family: Kinase

Novelty: 0.00374091

p_int: 0.874917456

p_ni: 8e-9

p_wrong: 0.125082536

Score: 0.546

Data Source: BioPlex,STRINGDB

CD320

Tbio

Novelty: 0.03078608

p_int: 0.857411228

p_ni: 0.142587369

p_wrong: 0.000001402

Score: 0.739

Data Source: BioPlex,STRINGDB

Publication Statistics

PubMed Score  317.67

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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Amino Acid Sequence

Residue Counts

Sequence

MVDGVMILPVLIMIALPSPSMEDEKPKVNPKLYMCVCEGLSCGNEDHCEGQQCFSSLSINDGFHVYQKGC

1-70

FQVYEQGKMTCKTPPSPGQAVECCQGDWCNRNITAQLPTKGKSFPGTQNFHLEVGLIILSVVFAVCLLAC

70-140

LLGVALRKFKRRNQERLNPRDVEYGTIEGLITTNVGDSTLADLLDHSCTSGSGSGLPFLVQRTVARQITL

140-210

LECVGKGRYGEVWRGSWQGENVAVKIFSSRDEKSWFRETELYNTVMLRHENILGFIASDMTSRHSSTQLW

210-280

LITHYHEMGSLYDYLQLTTLDTVSCLRIVLSIASGLAHLHIEIFGTQGKPAIAHRDLKSKNILVKKNGQC

280-350

CIADLGLAVMHSQSTNQLDVGNNPRVGTKRYMAPEVLDETIQVDCFDSYKRVDIWAFGLVLWEVARRMVS

350-420

NGIVEDYKPPFYDVVPNDPSFEDMRKVVCVDQQRPNIPNRWFSDPTLTSLAKLMKECWYQNPSARLTALR

420-490

IKKTLTKIDNSLDKLKTDC

490-509

MVDGVMILPVLIMIALPSPSMEDEKPKVNPKLYMCVCEGLSCGNEDHCEGQQCFSSLSINDGFHVYQKGCFQVYEQGKMTCKTPPSPGQAVECCQGDWCNRNITAQLPTKGKSFPGTQNFHLEVGLIILSVVFAVCLLACLLGVALRKFKRRNQERLNPRDVEYGTIEGLITTNVGDSTLADLLDHSCTSGSGSGLPFLVQRTVARQITLLECVGKGRYGEVWRGSWQGENVAVKIFSSRDEKSWFRETELYNTVMLRHENILGFIASDMTSRHSSTQLWLITHYHEMGSLYDYLQLTTLDTVSCLRIVLSIASGLAHLHIEIFGTQGKPAIAHRDLKSKNILVKKNGQCCIADLGLAVMHSQSTNQLDVGNNPRVGTKRYMAPEVLDETIQVDCFDSYKRVDIWAFGLVLWEVARRMVSNGIVEDYKPPFYDVVPNDPSFEDMRKVVCVDQQRPNIPNRWFSDPTLTSLAKLMKECWYQNPSARLTALRIKKTLTKIDNSLDKLKTDC

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Uniprot Keyword

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