BMP2 inducible kinase | Numb-associated kinase (NAK) family | IUPHAR/BPS Guide to PHARMACOLOGY

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BMP2 inducible kinase

Target not currently curated in GtoImmuPdb

Target id: 1941

Nomenclature: BMP2 inducible kinase

Abbreviated Name: BIKE

Family: Numb-associated kinase (NAK) family

Annotation status:  image of an orange circle Annotated and awaiting review. Please contact us if you can help with reviewing.  » Email us

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 662 4q21.21 BMP2K BMP2 inducible kinase
Mouse - 1138 5 E3 Bmp2k BMP2 inducible kinase
Rat - - 14p22 Bmp2k BMP-2 inducible kinase
Previous and Unofficial Names
BIKE
Database Links
BRENDA
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
Pharos
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Enzyme Reaction
EC Number: 2.7.11.1

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 Value Parameter Reference
baricitinib Hs Inhibition 7.4 pKd 3
pKd 7.4 (Kd 4x10-8 M) [3]
Description: Binding affinity determined in a cell-free biochemical assay.
compound 5m [PMID: 20483621] Hs Inhibition - - 2
[2]
Description: Measured as % inhibition using 1μM compound.
Inhibitor Comments
Compound 5m [PMID 20483621] inhibits BMP2K activity by approximately 84% using 1μM compound [2].
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: 1,4

Key to terms and symbols Click column headers to sort
Target used in screen: BIKE
Ligand Sp. Type Action Value Parameter
sunitinib Hs Inhibitor Inhibition 8.3 pKd
staurosporine Hs Inhibitor Inhibition 8.3 pKd
KW-2449 Hs Inhibitor Inhibition 8.0 pKd
lestaurtinib Hs Inhibitor Inhibition 7.8 pKd
SU-14813 Hs Inhibitor Inhibition 7.6 pKd
fedratinib Hs Inhibitor Inhibition 7.5 pKd
PHA-665752 Hs Inhibitor Inhibition 7.3 pKd
dovitinib Hs Inhibitor Inhibition 7.3 pKd
tozasertib Hs Inhibitor Inhibition 7.2 pKd
A-674563 Hs Inhibitor Inhibition 6.9 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »
Immuno Process Associations
Immuno Process:  Antigen presentation
GO Annotations:  Associated to 2 GO processes
GO:0030100 regulation of endocytosis IBA
GO:2000369 regulation of clathrin-dependent endocytosis IBA

References

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1. 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]

2. Milkiewicz KL, Weinberg LR, Albom MS, Angeles TS, Cheng M, Ghose AK, Roemmele RC, Theroff JP, Underiner TL, Zificsak CA et al.. (2010) Synthesis and structure-activity relationships of 1,2,3,4-tetrahydropyrido[2,3-b]pyrazines as potent and selective inhibitors of the anaplastic lymphoma kinase. Bioorg. Med. Chem., 18 (12): 4351-62. [PMID:20483621]

3. Stebbing J, Phelan A, Griffin I, Tucker C, Oechsle O, Smith D, Richardson P. (2020) COVID-19: combining antiviral and anti-inflammatory treatments. Lancet Infect Dis, 20 (4): 400-402. [PMID:32113509]

4. 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

Numb-associated kinase (NAK) family: BMP2 inducible kinase. Last modified on 09/03/2020. Accessed on 25/05/2020. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1941.