General Information of the Protein
Protein ID
PT01130
Protein Name
Activin receptor type-1B
Secondarily
Protein Name
Activin receptor type IB
Activin receptor-like kinase 4
Serine/threonine-protein kinase receptor R2
Gene Name
ACVR1B
Secondarily
Gene Name
ACVRLK4
ALK4
Sequence
MAESAGASSFFPLVVLLLAGSGGSGPRGVQALLCACTSCLQANYTCETDGACMVSIFNLDGMEHHVRTCIPKVELVPAGKPFYCLSSEDLRNTHCCYTDYCNRIDLRVPSGHLKEPEHPSMWGPVELVGIIAGPVFLLFLIIIIVFLVINYHQRVYHNRQRLDMEDPSCEMCLSKDKTLQDLVYDLSTSGSGSGLPLFVQRTVARTIVLQEIIGKGRFGEVWRGRWRGGDVAVKIFSSREERSWFREAEIYQTVMLRHENILGFIAADNKDNGTWTQLWLVSDYHEHGSLFDYLNRYTVTIEGMIKLALSAASGLAHLHMEIVGTQGKPGIAHRDLKSKNILVKKNGMCAIADLGLAVRHDAVTDTIDIAPNQRVGTKRYMAPEVLDETINMKHFDSFKCADIYALGLVYWEIARRCNSGGVHEEYQLPYYDLVPSDPSIEEMRKVVCDQKLRPNIPNWWQSYEALRVMGKMMRECWYANGAARLTALRIKKTLSQLSVQEDVKI
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Kinase
>
Protein Kinase
>
TKL protein kinase group
>
TKL protein kinase STKR family
>
TKL protein kinase STKR Type 1 subfamily
Function
Transmembrane serine/threonine kinase activin type-1 receptor forming an activin receptor complex with activin receptor type-2 (ACVR2A or ACVR2B). Transduces the activin signal from the cell surface to the cytoplasm and is thus regulating a many physiological and pathological processes including neuronal differentiation and neuronal survival, hair follicle development and cycling, FSH production by the pituitary gland, wound healing, extracellular matrix production, immunosuppression and carcinogenesis. Activin is also thought to have a paracrine or autocrine role in follicular development in the ovary. Within the receptor complex, type-2 receptors (ACVR2A and/or ACVR2B) act as a primary activin receptors whereas the type-1 receptors like ACVR1B act as downstream transducers of activin signals. Activin binds to type-2 receptor at the plasma membrane and activates its serine-threonine kinase. The activated receptor type-2 then phosphorylates and activates the type-1 receptor such as ACVR1B. Once activated, the type-1 receptor binds and phosphorylates the SMAD proteins SMAD2 and SMAD3, on serine residues of the C-terminal tail. Soon after their association with the activin receptor and subsequent phosphorylation, SMAD2 and SMAD3 are released into the cytoplasm where they interact with the common partner SMAD4. This SMAD complex translocates into the nucleus where it mediates activin-induced transcription. Inhibitory SMAD7, which is recruited to ACVR1B through FKBP1A, can prevent the association of SMAD2 and SMAD3 with the activin receptor complex, thereby blocking the activin signal. Activin signal transduction is also antagonized by the binding to the receptor of inhibin-B via the IGSF1 inhibin coreceptor. ACVR1B also phosphorylates TDP2.
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Uniprot ID
Primary ID:
P36896

Secondarily ID:
B7Z5L8
B7Z5W5
Q15479
Q15480
Q15481
Q15482
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Ensembl ID
ENSG00000135503
HGNC ID
HGNC:172
Subcellular Location
Cell membrane
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000006 , HEK293
Compound ID Compound Name Compound Formula
CP0505213
N,N-dimethyl-3-[5-[4-(5-pyridin-2-yl-1H-pyrazol-4-yl)pyridin-2-yl]pyridin-2-yl]oxypropan-1-amine
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C23H24N6O
 1
1
IC50 = 18 nM
   TI
   LI
   LO
   TS
CP0330405
N,N-dimethyl-2-[4-[4-(5-pyridin-2-yl-1H-pyrazol-4-yl)pyridin-2-yl]phenoxy]ethanamine
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C23H23N5O
 1
1
IC50 = 46 nM
   TI
   LI
   LO
   TS
CP0452298
1-methyl-4-[5-[4-(5-pyridin-2-yl-1H-pyrazol-4-yl)pyridin-2-yl]pyridin-2-yl]piperazine
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C23H23N7
 1
1
IC50 = 108 nM
   TI
   LI
   LO
   TS
CP0458349
2-(1-methylpyrazol-4-yl)-4-(5-pyridin-2-yl-1H-pyrazol-4-yl)pyridine
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C17H14N6
 1
1
IC50 = 224 nM
   TI
   LI
   LO
   TS
CP0482146
2-pyrazol-1-yl-4-(5-pyridin-2-yl-1H-pyrazol-4-yl)pyridine
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C16H12N6
 1
1
IC50 = 882 nM
   TI
   LI
   LO
   TS
CP0459894
2-imidazol-1-yl-4-(5-pyridin-2-yl-1H-pyrazol-4-yl)pyridine
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C16H12N6
 1
1
IC50 = 956 nM
   TI
   LI
   LO
   TS
CP0025391
4-(4-(3-(pyridin-2-yl)-1H-pyrazol-4-yl)pyridin-2-yl)-N-(tetrahydro-2H-pyran-4-yl)benzamide
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C25H23N5O2
 1
1
IC50 > 1000 nM
   TI
   LI
   LO
   TS
Clinical Information about the Protein
Target 1 ( Activin receptor type IB (ACVR1B) )
Target Type Patented-recorded Target