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ABL proto-oncogene 2, non-receptor tyrosine kinase

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Target not currently curated in GtoImmuPdb

Target id: 1924

Nomenclature: ABL proto-oncogene 2, non-receptor tyrosine kinase

Abbreviated Name: Arg

Family: Abl family

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 1182 1q25.2 ABL2 ABL proto-oncogene 2, non-receptor tyrosine kinase
Mouse - 1182 1 67.71 cM Abl2 ABL proto-oncogene 2, non-receptor tyrosine kinase
Rat - 1208 13q22 Abl2 ABL proto-oncogene 2, non-receptor tyrosine kinase
Previous and Unofficial Names Click here for help
Abelson-related gene | Abll | tyrosine-protein kinase ABL2 | c-abl oncogene 2, non-receptor tyrosine kinase | ABL proto-oncogene 2 | v-abl Abelson murine leukemia viral oncogene 2 (arg, Abelson-related gene) | v-abl Abelson murine leukemia viral oncogene 2 (arg
Database Links Click here for help
Alphafold P42684 (Hs), Q4JIM5 (Mm)
BRENDA 2.7.10.2
CATH/Gene3D 3.30.505.10
ChEMBL Target CHEMBL4014 (Hs), CHEMBL5222 (Mm)
Ensembl Gene ENSG00000143322 (Hs), ENSMUSG00000026596 (Mm), ENSRNOG00000004305 (Rn)
Entrez Gene 27 (Hs), 11352 (Mm), 304883 (Rn)
Human Protein Atlas ENSG00000143322 (Hs)
KEGG Enzyme 2.7.10.2
KEGG Gene hsa:27 (Hs), mmu:11352 (Mm), rno:304883 (Rn)
OMIM 164690 (Hs)
Pharos P42684 (Hs)
RefSeq Nucleotide NM_001136000 (Hs), NM_001136104 (Mm), NM_001107186 (Rn)
RefSeq Protein NP_005149 (Hs), NP_001129576 (Mm), NP_001100656 (Rn)
UniProtKB P42684 (Hs), Q4JIM5 (Mm)
Wikipedia ABL2 (Hs)
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  Human ABL2 in complex with AURORA Kinase inhibitor VX-680 (tozasertib).
PDB Id:  2XYN
Ligand:  tozasertib
Resolution:  2.81Å
Species:  Human
References:  6
Enzyme Reaction Click here for help
EC Number: 2.7.10.2

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 24 [PMID: 23441572] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.7 – 9.0 pIC50 4
⤷ pIC50 8.7 – 9.0 (IC50 2x10-9 – 1x10-9 M) [4]
pexmetinib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.0 pIC50 2
⤷ pIC50 8.0 (IC50 1x10-8 M) [2]
risvodetinib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.1 pIC50 7
⤷ pIC50 7.1 (IC50 7.7x10-8 M) [7]
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: 3,8
Key to terms and symbols Click column headers to sort
Target used in screen: ABL2
Ligand Sp. Type Action Value Parameter
dasatinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 9.8 pKd
PD-173955 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 9.2 pKd
bosutinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 8.8 pKd
AST-487 Small molecule or natural product Hs Inhibitor Inhibition 8.5 pKd
tozasertib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.4 pKd
imatinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 8.0 pKd
nilotinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 7.6 pKd
foretinib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.6 pKd
vandetanib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 7.2 pKd
axitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 7.2 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »
EMD Millipore KinaseProfilerTM screen/Reaction Biology Kinase HotspotSM screen Click here for help
A screen profiling 158 kinase inhibitors (Calbiochem Protein Kinase Inhibitor Library I and II, catalogue numbers 539744 and 539745) for their inhibitory activity at 1µM and 10µM against 234 human recombinant kinases using the EMD Millipore KinaseProfilerTM service.

A screen profiling the inhibitory activity of 178 commercially available kinase inhibitors at 0.5µM against a panel of 300 recombinant protein kinases using the Reaction Biology Corporation Kinase HotspotSM platform.

http://www.millipore.com/techpublications/tech1/pf3036
http://www.reactionbiology.com/webapps/main/pages/kinase.aspx

Reference: 1,5
Key to terms and symbols Click column headers to sort
Target used in screen: Arg/ABL2(ARG)
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
TWS119 Small molecule or natural product Hs Inhibitor Inhibition 1.4 -3.0 -2.0
bosutinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 2.2
dasatinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 2.7
nilotinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 4.9
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 5.3 3.5 -1.0
tozasertib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 5.7
GSK-3 inhibitor IX Small molecule or natural product Hs Inhibitor Inhibition 8.4 16.0 2.0
Cdk1/2 inhibitor III Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 10.5 -2.0 -2.0
dorsomorphin Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 13.6 12.0 1.0
vandetanib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 14.0
Displaying the top 10 most potent ligands  View all ligands in screen »
Immuno Process Associations
Immuno Process:  Antigen presentation
Immuno Process:  Cellular signalling
Immuno Process:  Cytokine production & signalling
Immuno Process:  Immune system development
Immuno Process:  Inflammation
Immuno Process:  T cell (activation)

References

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1. Anastassiadis T, Deacon SW, Devarajan K, Ma H, Peterson JR. (2011) Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity. Nat Biotechnol, 29 (11): 1039-45. [PMID:22037377]

2. Bachegowda L, Morrone K, Winski SL, Mantzaris I, Bartenstein M, Ramachandra N, Giricz O, Sukrithan V, Nwankwo G, Shahnaz S et al.. (2016) Pexmetinib: A Novel Dual Inhibitor of Tie2 and p38 MAPK with Efficacy in Preclinical Models of Myelodysplastic Syndromes and Acute Myeloid Leukemia. Cancer Res, 76 (16): 4841-4849. [PMID:27287719]

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. Desai B, Dixon K, Farrant E, Feng Q, Gibson KR, van Hoorn WP, Mills J, Morgan T, Parry DM, Ramjee MK et al.. (2013) Rapid discovery of a novel series of Abl kinase inhibitors by application of an integrated microfluidic synthesis and screening platform. J Med Chem, 56 (7): 3033-47. [PMID:23441572]

5. Gao Y, Davies SP, Augustin M, Woodward A, Patel UA, Kovelman R, Harvey KJ. (2013) A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. Biochem J, 451 (2): 313-28. [PMID:23398362]

6. Salah E, Ugochukwu E, Barr AJ, von Delft F, Knapp S, Elkins JM. (2011) Crystal structures of ABL-related gene (ABL2) in complex with imatinib, tozasertib (VX-680), and a type I inhibitor of the triazole carbothioamide class. J Med Chem, 54 (7): 2359-67. [PMID:21417343]

7. Werner MH, Kelly TA. (2020) Compositions and methods for inhibiting kinases. Patent number: US20200046699A1. Assignee: Inhibikase Therapeutics Inc. Priority date: 25/10/2017. Publication date: 13/02/2020.

8. 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

Abl family: ABL proto-oncogene 2, non-receptor tyrosine kinase. Last modified on 21/02/2023. Accessed on 06/12/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetoimmunopharmacology.org/GRAC/ObjectDisplayForward?objectId=1924.