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BMP2 inducible kinase

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Target not currently curated in GtoImmuPdb

Target id: 1941

Nomenclature: BMP2 inducible kinase

Abbreviated Name: BIKE

Family: Numb-associated kinase (NAK) family

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 1161 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 Click here for help
BIKE
Database Links Click here for help
Alphafold Q9NSY1 (Hs), Q91Z96 (Mm)
BRENDA 2.7.11.1
ChEMBL Target CHEMBL4522 (Hs)
Ensembl Gene ENSG00000138756 (Hs), ENSMUSG00000034663 (Mm), ENSRNOG00000002040 (Rn)
Entrez Gene 55589 (Hs), 140780 (Mm), 498333 (Rn)
Human Protein Atlas ENSG00000138756 (Hs)
KEGG Enzyme 2.7.11.1
KEGG Gene hsa:55589 (Hs), mmu:140780 (Mm), rno:498333 (Rn)
Pharos Q9NSY1 (Hs)
RefSeq Nucleotide NM_017593 (Hs), NM_080708 (Mm)
RefSeq Protein NP_060063 (Hs), NP_542439 (Mm)
UniProtKB Q9NSY1 (Hs), Q91Z96 (Mm)
Wikipedia BMP2K (Hs)
Enzyme Reaction Click here for help
EC Number: 2.7.11.1

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
baricitinib Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 7.4 pKd 4
⤷ pKd 7.4 (Kd 4x10-8 M) [4]
Description: Binding affinity determined in a cell-free biochemical assay.
compound 6 [PMID: 34333981] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.4 pIC50 2
⤷ pIC50 7.4 (IC50 3.8x10-8 M) [2]
compound 13 [PMID: 34333981] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.4 pIC50 2
⤷ pIC50 7.4 (IC50 4x10-8 M) [2]
compound 5m [PMID: 20483621] Small molecule or natural product Click here for species-specific activity table Hs Inhibition - - 3
⤷ [3]
Description: Measured as % inhibition using 1μM compound.
Inhibitor Comments
Compound 5m [PMID 20483621] inhibits BMP2K activity by approximately 84% using 1μM compound [3].
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: 1,5
Key to terms and symbols Click column headers to sort
Target used in screen: BIKE
Ligand Sp. Type Action Value Parameter
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 8.3 pKd
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.3 pKd
KW-2449 Small molecule or natural product Hs Inhibitor Inhibition 8.0 pKd
lestaurtinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 7.8 pKd
SU-14813 Small molecule or natural product Hs Inhibitor Inhibition 7.6 pKd
fedratinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 7.5 pKd
PHA-665752 Small molecule or natural product Hs Inhibitor Inhibition 7.3 pKd
dovitinib Small molecule or natural product Hs Inhibitor Inhibition 7.3 pKd
tozasertib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.2 pKd
A-674563 Small molecule or natural product Ligand has a PDB structure 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

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. Drewry DH, Annor-Gyamfi JK, Wells CI, Pickett JE, Dederer V, Preuss F, Mathea S, Axtman AD. (2022) Identification of Pyrimidine-Based Lead Compounds for Understudied Kinases Implicated in Driving Neurodegeneration. J Med Chem, 65 (2): 1313-1328. [PMID:34333981]

3. 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]

4. 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]

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]

How to cite this page

Numb-associated kinase (NAK) family: BMP2 inducible kinase. Last modified on 08/02/2022. Accessed on 14/10/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetoimmunopharmacology.org/GRAC/ObjectDisplayForward?objectId=1941.