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

bone morphogenetic protein receptor type IB

Target id: 1789

Nomenclature: bone morphogenetic protein receptor type IB

Abbreviated Name: BMPR1B

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 IB 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 1 502 4q23-q24 BMPR1B bone morphogenetic protein receptor type 1B
Mouse 1 502 3 Bmpr1b bone morphogenetic protein receptor, type 1B
Rat - 297 2q44 Bmpr1b bone morphogenetic protein receptor type 1B
Previous and Unofficial Names
Activin receptor-like kinase 6 | Acvrlk6 | ALK6 | BMP receptor IB | BMPR-IB | bone morphogenetic protein receptor | Serine/threonine-protein kinase receptor R6 | SKR6
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 the cytoplasmic domain of the bone morphogenetic protein receptor type-1B (BMPR1B) in complex with FKBP12 and LDN-193189
PDB Id:  3MDY
Resolution:  2.05Å
Species:  Human
References: 
Enzyme Reaction
EC Number: 2.7.11.30
Natural/Endogenous Ligands
growth/differentiation factor-5 {Sp: Human}
Comments: 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 7.2 pIC50 3
pIC50 7.2 (IC50 6.09x10-8 M) [3]
galunisertib Hs Inhibition 6.3 pIC50 6
pIC50 6.3 (IC50 4.71x10-7 M) [6]
Description: Value determined usinfg the DiscoverX KINOMEscan platform.
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: BMPR1B
Ligand Sp. Type Action Affinity Units
NVP-TAE684 Hs Inhibitor Inhibition 9.1 pKd
PP-242 Hs Inhibitor Inhibition 8.7 pKd
PD-173955 Hs Inhibitor Inhibition 8.4 pKd
dasatinib Hs Inhibitor Inhibition 7.3 pKd
lestaurtinib Hs Inhibitor Inhibition 7.2 pKd
KW-2449 Hs Inhibitor Inhibition 6.9 pKd
staurosporine Hs Inhibitor Inhibition 6.8 pKd
crizotinib Hs Inhibitor Inhibition 6.6 pKd
vandetanib Hs Inhibitor Inhibition 6.6 pKd
JNJ-28312141 Hs Inhibitor Inhibition 6.4 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »
Clinically-Relevant Mutations and Pathophysiology
Disease:  Brachydactyly, type A2; BDA2
Synonyms: Brachydactyly [Disease Ontology: DOID:0050581]
Disease Ontology: DOID:0050581
OMIM: 112600
Orphanet: ORPHA93396
Disease:  Brachydactyly, type C; BDC
Synonyms: Brachydactyly [Disease Ontology: DOID:0050581]
Disease Ontology: DOID:0050581
OMIM: 113100
Orphanet: ORPHA93384
References:  4
Disease:  Chondrodysplasia, acromesomelic, with genital anomalies
OMIM: 609441

References

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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. Lehmann K, Seemann P, Boergermann J, Morin G, Reif S, Knaus P, Mundlos S. (2006) A novel R486Q mutation in BMPR1B resulting in either a brachydactyly type C/symphalangism-like phenotype or brachydactyly type A2. Eur. J. Hum. Genet., 14 (12): 1248-54. [PMID:16957682]

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]

6. 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: bone morphogenetic protein receptor type IB. Last modified on 16/08/2018. Accessed on 14/11/2018. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1789.