bone morphogenetic protein receptor type IA | Type I receptor serine/threonine kinases | IUPHAR/BPS Guide to PHARMACOLOGY

bone morphogenetic protein receptor type IA

Target id: 1786

Nomenclature: bone morphogenetic protein receptor type IA

Abbreviated Name: BMPR1A

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

   GtoImmuPdb view: OFF :     Currently no data for bone morphogenetic protein receptor type IA in GtoImmuPdb

Quaternary Structure: Complexes
Bone morphogenetic protein receptors
Growth/differentiation factor receptors
Anti-Müllerian hormone receptors
Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 1 532 10q22.3 BMPR1A bone morphogenetic protein receptor type 1A
Mouse 1 532 14 Bmpr1a bone morphogenetic protein receptor, type 1A
Rat 1 532 16p16 Bmpr1a bone morphogenetic protein receptor type 1A
Previous and Unofficial Names
BMP receptor IA | CD292 | SKR5 | activin receptor-like kinase 3 | bone morphogenetic protein 4 receptor | BMP-2/BMP-4 receptor | ALK3 | ACVRLK3 | serine/threonine-protein kinase receptor R5 | bone morphogenetic protein receptor
Database Links
BRENDA
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Orphanet
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of a TGF-beta ligand-receptor complex between growth/differentiation factor 5 and bone morphogenetic protein receptor type-1A
PDB Id:  3QB4
Resolution:  2.28Å
Species:  Human
References: 
Enzyme Reaction
EC Number: 2.7.11.30
Natural/Endogenous Ligands
Müllerian inhibiting substance {Sp: Human}
Comments: Other endogenous ligands may include growth/differentiation factor-6 [1].

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 Affinity Units Reference
compound 13d [PMID: 23639540] Hs Inhibition >8.3 pIC50 3
pIC50 >8.3 (IC50 <5x10-9 M) [3]
compound 13r [PMID: 23639540] Hs Inhibition >8.3 pIC50 3
pIC50 >8.3 (IC50 <5x10-9 M) [3]
compound 13a [PMID: 23639540] Hs Inhibition 8.0 pIC50 3
pIC50 8.0 (IC50 1.04x10-8 M) [3]
LDN-214117 Hs Inhibition 5.9 pIC50 4
pIC50 5.9 (IC50 1.171x10-6 M) [4]
ML347 Hs Inhibition 5.0 pIC50 3
pIC50 5.0 (IC50 1.08x10-5 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: 2,5

Key to terms and symbols Click column headers to sort
Target used in screen: BMPR1A
Ligand Sp. Type Action Affinity Units
PP-242 Hs Inhibitor Inhibition 7.2 pKd
PD-173955 Hs Inhibitor Inhibition 6.8 pKd
NVP-TAE684 Hs Inhibitor Inhibition 6.8 pKd
lestaurtinib Hs Inhibitor Inhibition 6.0 pKd
KW-2449 Hs Inhibitor Inhibition 5.7 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
masitinib Hs Inhibitor Inhibition <5.5 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »
Clinically-Relevant Mutations and Pathophysiology
Disease:  Chromosome 10q23 deletion syndrome
Synonyms: Juvenile polyposis of infancy [Orphanet: ORPHA79076]
OMIM: 612242
Orphanet: ORPHA79076
Disease:  Generalized juvenile polyposis/juvenile polyposis coli
Synonyms: Juvenile polypolis syndrome; JPS [OMIM: 174900]
OMIM: 174900
Orphanet: ORPHA329971
Disease:  Hereditary nonpolyposis colon cancer
Orphanet: ORPHA144
Disease:  Polyposis syndrome, hereditary mixed, 2; HMPS2
OMIM: 610069
Orphanet: ORPHA157794

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. 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. Mohedas AH, Wang Y, Sanvitale CE, Canning P, Choi S, Xing X, Bullock AN, Cuny GD, Yu PB. (2014) Structure-activity relationship of 3,5-diaryl-2-aminopyridine ALK2 inhibitors reveals unaltered binding affinity for fibrodysplasia ossificans progressiva causing mutants. J. Med. Chem., 57 (19): 7900-15. [PMID:25101911]

5. 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 I receptor serine/threonine kinases: bone morphogenetic protein receptor type IA. Last modified on 10/07/2018. Accessed on 15/11/2018. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1786.