activin A receptor type 1B | Type I receptor serine/threonine kinases | IUPHAR/BPS Guide to PHARMACOLOGY

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activin A receptor type 1B

Target not currently curated in GtoImmuPdb

Target id: 1787

Nomenclature: activin A receptor type 1B

Abbreviated Name: ALK4

Family: Type I 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
Growth/differentiation factor receptors
Activin receptors
Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 1 505 12q13 ACVR1B activin A receptor type 1B
Mouse 1 505 15 Acvr1b activin A receptor, type 1B
Rat 1 505 7q35 Acvr1b activin A receptor type 1B
Previous and Unofficial Names
activin A receptor | activin A receptor type IB | activin receptor-like kinase 4 | ActR-IB | ActRIB | ACVRLK4 | Alk4 | serine/threonine-protein kinase receptor R2 | SKR2
Database Links
BRENDA
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Enzyme Reaction
EC Number: 2.7.11.30
Natural/Endogenous Ligands
growth/differentiation factor-11 {Sp: Human}

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

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
vactosertib Hs Inhibition 7.9 pIC50 5
pIC50 7.9 (IC50 1.3x10-8 M) [5]
Description: Measured using Reaction Biology Corporation's HotSpot kinase assay
galunisertib Hs Inhibition 7.1 pIC50 7
pIC50 7.1 (IC50 7.8x10-8 M) [7]
Description: Value determined usinfg the DiscoverX KINOMEscan platform.
compound 13r [PMID: 23639540] Hs Inhibition 6.7 pIC50 3
pIC50 6.7 (IC50 1.83x10-7 M) [3]
compound 13d [PMID: 23639540] Hs Inhibition 6.5 pIC50 3
pIC50 6.5 (IC50 3.26x10-7 M) [3]
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: 2,6

Key to terms and symbols Click column headers to sort
Target used in screen: ACVR1B
Ligand Sp. Type Action Value Parameter
JNJ-28312141 Hs Inhibitor Inhibition 8.0 pKd
PP-242 Hs Inhibitor Inhibition 7.2 pKd
lestaurtinib Hs Inhibitor Inhibition 7.1 pKd
PD-173955 Hs Inhibitor Inhibition 7.0 pKd
NVP-TAE684 Hs Inhibitor Inhibition 7.0 pKd
dasatinib Hs Inhibitor Inhibition 6.5 pKd
staurosporine Hs Inhibitor Inhibition 6.2 pKd
crizotinib Hs Inhibitor Inhibition 6.1 pKd
tamatinib Hs Inhibitor Inhibition 6.0 pKd
cediranib Hs Inhibitor Inhibition 5.8 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »
EMD Millipore KinaseProfilerTM screen/Reaction Biology Kinase HotspotSM screen
A screen profiling 158 kinase inhibitors (Calbiochem Protein Kinase Inhibitor Library I and II, catalogue numbers 539744 and 539745) for their inhibitory activity at 1µM and 10µM against 234 human recombinant kinases using the EMD Millipore KinaseProfilerTM service.

A screen profiling the inhibitory activity of 178 commercially available kinase inhibitors at 0.5µM against a panel of 300 recombinant protein kinases using the Reaction Biology Corporation Kinase HotspotSM platform.

http://www.millipore.com/techpublications/tech1/pf3036
http://www.reactionbiology.com/webapps/main/pages/kinase.aspx


Reference: 1,4

Key to terms and symbols Click column headers to sort
Target used in screen: nd/ALK4(ACVR1B)
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
TGF-beta RI inhibitor III Hs Inhibitor Inhibition 31.0 1.0 -6.0
TGF-beta RI kinase inhibitor Hs Inhibitor Inhibition 43.2 -3.0 -4.0
SB 202474 Hs Inhibitor Inhibition 86.5 94.0 97.0
SKI II Hs Inhibitor Inhibition 89.5 104.0 110.0
PDGF RTK inhibitor Hs Inhibitor Inhibition 92.1 126.0 96.0
Cdk1/2 inhibitor III Hs Inhibitor Inhibition 92.2 7.0 -4.0
PD98059 Hs Inhibitor Inhibition 92.5 111.0 108.0
mubritinib Hs Inhibitor Inhibition 92.8
PDGF receptor tyrosine kinase inhibitor IV Hs Inhibitor Inhibition 92.9 117.0 91.0
KN-93 Hs Inhibitor Inhibition 93.2 96.0 102.0
Displaying the top 10 most potent ligands  View all ligands in screen »

References

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1. Anastassiadis T, Deacon SW, Devarajan K, Ma H, Peterson JR. (2011) Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity. Nat. Biotechnol., 29 (11): 1039-45. [PMID:22037377]

2. 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]

3. Engers DW, Frist AY, Lindsley CW, Hong CC, Hopkins CR. (2013) Synthesis and structure-activity relationships of a novel and selective bone morphogenetic protein receptor (BMP) inhibitor derived from the pyrazolo[1.5-a]pyrimidine scaffold of dorsomorphin: the discovery of ML347 as an ALK2 versus ALK3 selective MLPCN probe. Bioorg. Med. Chem. Lett., 23 (11): 3248-52. [PMID:23639540]

4. Gao Y, Davies SP, Augustin M, Woodward A, Patel UA, Kovelman R, Harvey KJ. (2013) A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. Biochem. J., 451 (2): 313-28. [PMID:23398362]

5. Jin CH, Krishnaiah M, Sreenu D, Subrahmanyam VB, Rao KS, Lee HJ, Park SJ, Park HJ, Lee K, Sheen YY et al.. (2014) Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/antifibrotic agent. J. Med. Chem., 57 (10): 4213-38. [PMID:24786585]

6. 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]

7. Yingling JM, McMillen WT, Yan L, Huang H, Sawyer JS, Graff J, Clawson DK, Britt KS, Anderson BD, Beight DW et al.. (2018) Preclinical assessment of galunisertib (LY2157299 monohydrate), a first-in-class transforming growth factor-β receptor type I inhibitor. Oncotarget, 9 (6): 6659-6677. [PMID:29467918]

How to cite this page

Type I receptor serine/threonine kinases: activin A receptor type 1B. Last modified on 16/08/2018. Accessed on 18/07/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1787.