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bone morphogenetic protein receptor type IB

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Target not currently curated in GtoImmuPdb

Target id: 1789

Nomenclature: bone morphogenetic protein receptor type IB

Abbreviated Name: BMPR1B

Family: Type I receptor serine/threonine kinases

Contents:

Quaternary Structure: Complexes
Bone morphogenetic protein receptors
Growth/differentiation factor receptors
Anti-Müllerian hormone receptors
Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 1 502 4q22.3 BMPR1B bone morphogenetic protein receptor type 1B
Mouse 1 502 3 H1 Bmpr1b bone morphogenetic protein receptor, type 1B
Rat - 297 2q44 Bmpr1b bone morphogenetic protein receptor type 1B
Previous and Unofficial Names Click here for help
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 Click here for help
Alphafold O00238 (Hs), P36898 (Mm)
BRENDA 2.7.11.30
ChEMBL Target CHEMBL5476 (Hs)
Ensembl Gene ENSG00000138696 (Hs), ENSMUSG00000052430 (Mm), ENSRNOG00000016289 (Rn)
Entrez Gene 658 (Hs), 12167 (Mm), 310914 (Rn)
Human Protein Atlas ENSG00000138696 (Hs)
KEGG Enzyme 2.7.11.30
KEGG Gene hsa:658 (Hs), mmu:12167 (Mm), rno:310914 (Rn)
OMIM 603248 (Hs)
Orphanet ORPHA119053 (Hs)
Pharos O00238 (Hs)
RefSeq Nucleotide NM_001203 (Hs), NM_007560 (Mm), NM_001024259 (Rn)
RefSeq Protein NP_001194 (Hs), NP_031586 (Mm), NP_001019430 (Rn)
UniProtKB O00238 (Hs), P36898 (Mm)
Wikipedia BMPR1B (Hs)
Selected 3D Structures Click here for help
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 Click here for help
EC Number: 2.7.11.30
Natural/Endogenous Ligands Click here for help
growth/differentiation factor-5 {Sp: Human}
Comments: Endogenous ligands may include growth/differentiation factor-6 [2].

Download all structure-activity data for this target as a CSV file go icon to follow link

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
compound 13d [PMID: 23639540] Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition >8.3 pIC50 4
⤷ pIC50 >8.3 (IC50 <5x10-9 M) [4]
compound 13r [PMID: 23639540] Small molecule or natural product Click here for species-specific activity table Hs Inhibition >8.3 pIC50 4
⤷ pIC50 >8.3 (IC50 <5x10-9 M) [4]
compound 13a [PMID: 23639540] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.2 pIC50 4
⤷ pIC50 7.2 (IC50 6.09x10-8 M) [4]
galunisertib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.3 pIC50 7
⤷ pIC50 6.3 (IC50 4.71x10-7 M) [7]
Description: Value determined usinfg the DiscoverX KINOMEscan platform.
zilurgisertib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 5.5 pIC50 1
⤷ pIC50 5.5 (IC50 3.3x10-6 M) [1]
DiscoveRx KINOMEscan® screen Click here for help
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: 3,6
Key to terms and symbols Click column headers to sort
Target used in screen: BMPR1B
Ligand Sp. Type Action Value Parameter
NVP-TAE684 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 9.1 pKd
PP-242 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.7 pKd
PD-173955 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.4 pKd
dasatinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 7.3 pKd
lestaurtinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 7.2 pKd
KW-2449 Small molecule or natural product Hs Inhibitor Inhibition 6.9 pKd
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.8 pKd
crizotinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.6 pKd
vandetanib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 6.6 pKd
JNJ-28312141 Small molecule or natural product Hs Inhibitor Inhibition 6.4 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »
Clinically-Relevant Mutations and Pathophysiology Click here for help
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:  5
Disease:  Chondrodysplasia, acromesomelic, with genital anomalies
OMIM: 609441

References

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1. Arista L, Babu S, Bian J, Cui K, Dillon MP, Lattmann R, Li J, Liao L, Lizos D, Ramos R et al.. (2021) Aminopyridine derivatives and their use as selective alk-2 inhibitors. Patent number: US20210155606A1. Assignee: Novartis AG. Priority date: 20/07/2016. Publication date: 27/05/2021.

2. 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]

3. 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]

4. 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]

5. 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]

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: bone morphogenetic protein receptor type IB. Last modified on 04/02/2022. Accessed on 04/12/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetoimmunopharmacology.org/GRAC/ObjectDisplayForward?objectId=1789.