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

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bone morphogenetic protein receptor type IB

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

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
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
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
RefSeq Nucleotide
RefSeq Protein
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
Resolution:  2.05Å
Species:  Human
Enzyme Reaction
EC Number:
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

Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter 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.
Reference: 2,5

Key to terms and symbols Click column headers to sort
Target used in screen: BMPR1B
Ligand Sp. Type Action Value Parameter
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 »
Immuno Process Associations
Immuno Process:  Inflammation
GO Annotations:  Associated to 1 GO processes, IEA only
click arrow to show/hide IEA associations
GO:0006954 inflammatory response IEA
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


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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 01/10/2020. IUPHAR/BPS Guide to PHARMACOLOGY,