ABL proto-oncogene 2, non-receptor tyrosine kinase | Abl family | IUPHAR/BPS Guide to PHARMACOLOGY

Top ▲

ABL proto-oncogene 2, non-receptor tyrosine kinase

Target not currently curated in GtoImmuPdb

Target id: 1924

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

Abbreviated Name: Arg

Family: Abl 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 - 1167 1q25.2 ABL2 ABL proto-oncogene 2, non-receptor tyrosine kinase
Mouse - 1078 1 G3-H1 Abl2 v-abl Abelson murine leukemia viral oncogene 2 (arg, Abelson-related gene)
Rat - 1208 13q22 Abl2 ABL proto-oncogene 2, non-receptor tyrosine kinase
Previous and Unofficial Names
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
BRENDA
CATH/Gene3D
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Selected 3D Structures
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
EC Number: 2.7.10.2

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
compound 24 [PMID: 23441572] Hs Inhibition 8.7 – 9.0 pIC50 4
pIC50 8.7 – 9.0 (IC50 2x10-9 – 1x10-9 M) [4]
pexmetinib Hs Inhibition 8.0 pIC50 2
pIC50 8.0 (IC50 1x10-8 M) [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: 3,7

Key to terms and symbols Click column headers to sort
Target used in screen: ABL2
Ligand Sp. Type Action Value Parameter
dasatinib Hs Inhibitor Inhibition 9.8 pKd
PD-173955 Hs Inhibitor Inhibition 9.2 pKd
bosutinib Hs Inhibitor Inhibition 8.8 pKd
AST-487 Hs Inhibitor Inhibition 8.5 pKd
tozasertib Hs Inhibitor Inhibition 8.4 pKd
imatinib Hs Inhibitor Inhibition 8.0 pKd
nilotinib Hs Inhibitor Inhibition 7.6 pKd
foretinib Hs Inhibitor Inhibition 7.6 pKd
vandetanib Hs Inhibitor Inhibition 7.2 pKd
axitinib 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
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 Hs Inhibitor Inhibition 1.4 -3.0 -2.0
bosutinib Hs Inhibitor Inhibition 2.2
dasatinib Hs Inhibitor Inhibition 2.7
nilotinib Hs Inhibitor Inhibition 4.9
staurosporine Hs Inhibitor Inhibition 5.3 3.5 -1.0
tozasertib Hs Inhibitor Inhibition 5.7
GSK-3 inhibitor IX Hs Inhibitor Inhibition 8.4 16.0 2.0
Cdk1/2 inhibitor III Hs Inhibitor Inhibition 10.5 -2.0 -2.0
dorsomorphin Hs Inhibitor Inhibition 13.6 12.0 1.0
vandetanib Hs Inhibitor Inhibition 14.0
Displaying the top 10 most potent ligands  View all ligands in screen »

References

Show »

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. 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 24/04/2018. Accessed on 10/12/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1924.