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
Database Links
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
RefSeq Nucleotide
RefSeq Protein
Enzyme Reaction
EC Number:

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
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
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.
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


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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 12/07/2020. IUPHAR/BPS Guide to PHARMACOLOGY,