ABL proto-oncogene 1, non-receptor tyrosine kinase | Abl family | IUPHAR/BPS Guide to PHARMACOLOGY

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ABL proto-oncogene 1, non-receptor tyrosine kinase

Target id: 1923

Nomenclature: ABL proto-oncogene 1, non-receptor tyrosine kinase

Abbreviated Name: Abl

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

   GtoImmuPdb view: OFF :     ABL proto-oncogene 1, non-receptor tyrosine kinase has curated data in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 1130 9q34.1 ABL1 ABL proto-oncogene 1, non-receptor tyrosine kinase
Mouse - 1142 2 B Abl1 c-abl oncogene 1, non-receptor tyrosine kinase
Rat - 1143 3p12 Abl1 ABL proto-oncogene 1, non-receptor tyrosine kinase
Previous and Unofficial Names
JTK7 | Ab | Abelson murine leukemia viral (v-abl) oncogene homolog 1 | tyrosine-protein kinase ABL1 | ABL proto-oncogene 1
Database Links
BRENDA
CATH/Gene3D
DrugBank Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Orphanet
RefSeq Nucleotide
RefSeq Protein
SynPHARM
UniProtKB
Wikipedia
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  CRYSTAL STRUCTURE OF THE ABL-SH3 DOMAIN COMPLEXED WITH A DESIGNED HIGH-AFFINITY PEPTIDE LIGAND: IMPLICATIONS FOR SH3-LIGAND INTERACTIONS
PDB Id:  1BBZ
Resolution:  1.65Å
Species:  Human
References:  22
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of the c-Abl kinase domain in complex with INNO-406
PDB Id:  2E2B
Ligand:  bafetinib
Resolution:  2.2Å
Species:  Human
References:  13
Image of receptor 3D structure from RCSB PDB
Description:  The crystal structure of human abl1 kinase domain in complex with DCC-2036
PDB Id:  3QRI
Ligand:  rebastinib
Resolution:  2.1Å
Species:  Human
References:  4
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 Affinity Units Reference
PD-173955 Hs Inhibition 9.2 pKd 6
pKd 9.2 (Kd 5.8x10-10 M) [6]
BO1 Hs Inhibition 7.0 – 7.4 pKi 5,23
pKi 7.0 – 7.4 (Ki 1x10-7 – 4.4x10-8 M) [5,23]
compound 8h [PMID: 21561767] Hs Inhibition 9.7 pIC50 25
pIC50 9.7 (IC50 2x10-10 M) [25]
dasatinib Hs Inhibition 9.6 pIC50 16
pIC50 9.6 (IC50 2.7x10-10 M) [16]
PF-114 Hs Inhibition 9.3 pIC50 18
pIC50 9.3 (IC50 4.9x10-10 M) [18]
Description: Inhibition of native ABL kinase activity.
compound 24 [PMID: 23441572] Hs Inhibition 9.3 pIC50 7
pIC50 9.3 (IC50 5x10-10 M) [7]
rebastinib Hs Inhibition 9.1 pIC50 4,21
pIC50 9.1 (IC50 8x10-10 M) [4,21]
bosutinib Hs Inhibition 9.0 pIC50 11
pIC50 9.0 (IC50 1x10-9 M) [11]
compound 2c [PMID: 24900538] Hs Inhibition 8.9 pIC50 26
pIC50 8.9 (IC50 1.2x10-9 M) [26]
flumatinib Hs Inhibition 8.9 pIC50 17
pIC50 8.9 (IC50 1.2x10-9 M) [17]
pexmetinib Hs Inhibition 8.4 pIC50 3
pIC50 8.4 (IC50 4x10-9 M) [3]
PD-173955 Hs Inhibition ~8.3 pIC50 19
pIC50 ~8.3 (IC50 ~5x10-9 M) [19]
ponatinib Hs Inhibition 8.1 pIC50 14
pIC50 8.1 (IC50 8.6x10-9 M) [14]
bafetinib Hs Inhibition 7.6 – 8.2 pIC50 13,15
pIC50 7.6 – 8.2 (IC50 2.6x10-8 – 5.8x10-9 M) [13,15]
KW-2449 Hs Inhibition 7.8 pIC50 24
pIC50 7.8 (IC50 1.4x10-8 M) [24]
nilotinib Hs Inhibition 7.8 pIC50 20
pIC50 7.8 (IC50 1.5x10-8 M) [20]
PP121 Hs Inhibition 7.7 pIC50 2
pIC50 7.7 (IC50 1.8x10-8 M) [2]
saracatinib Hs Inhibition 7.5 pIC50 12
pIC50 7.5 (IC50 3x10-8 M) [12]
imatinib Hs Inhibition 6.7 pIC50 13
pIC50 6.7 (IC50 2.2x10-7 M) [13]
GNF-5 Hs Inhibition 6.7 pIC50 28
pIC50 6.7 (IC50 2.2x10-7 M) [28]
Description: Inhibition of wild-type Abl in vitro.
eCF506 Hs Inhibition 6.3 pIC50 9
pIC50 6.3 (IC50 4.79x10-7 M) [9]
Inhibitor Comments
Note that bosutinib has inhibitory activity at other kinases including HCK, LYN and Src.
KW-2449 inhibits Abl1T315I with IC50 of 4nM [24].
Compound 24 [PMID 23441572] inhibits Abl1T315I, Abl1H396P, Abl1Q252H, Abl1M351T and Abl1Y253F with IC50 values between 0.3-0.5nM [7].
Compound 8h [PMID 21561767] inhibits Abl1T315I with IC50 of 0.4nM [25].
Allosteric Modulators
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
asciminib Hs Negative 8.6 – 9.5 pIC50 8
pIC50 8.6 – 9.5 (IC50 2.4x10-9 – 3x10-10 M) [8]
Description: Two assays used: a radiometric filter-binding assay and microfluidic mobility shift technology (Caliper assay).
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: 6,27

Key to terms and symbols Click column headers to sort
Target used in screen: ABL1(E255K)-phosphorylated
Ligand Sp. Type Action Affinity Units
bosutinib Hs Inhibitor Inhibition 10.3 pKd
dasatinib Hs Inhibitor Inhibition 10.3 pKd
PD-173955 Hs Inhibitor Inhibition 9.3 pKd
tozasertib Hs Inhibitor Inhibition 8.5 pKd
vandetanib Hs Inhibitor Inhibition 7.9 pKd
staurosporine Hs Inhibitor Inhibition 7.7 pKd
canertinib Hs Inhibitor Inhibition 7.5 pKd
nilotinib Hs Inhibitor Inhibition 7.4 pKd
KW-2449 Hs Inhibitor Inhibition 7.4 pKd
fedratinib Hs Inhibitor Inhibition 7.4 pKd
Target used in screen: ABL1(F317I)-nonphosphorylated
Ligand Sp. Type Action Affinity Units
dasatinib Hs Inhibitor Inhibition 10.0 pKd
bosutinib Hs Inhibitor Inhibition 9.2 pKd
AST-487 Hs Inhibitor Inhibition 8.7 pKd
PD-173955 Hs Inhibitor Inhibition 8.3 pKd
masitinib Hs Inhibitor Inhibition 8.1 pKd
imatinib Hs Inhibitor Inhibition 8.1 pKd
nilotinib Hs Inhibitor Inhibition 7.7 pKd
foretinib Hs Inhibitor Inhibition 7.4 pKd
NVP-TAE684 Hs Inhibitor Inhibition 7.0 pKd
staurosporine Hs Inhibitor Inhibition 6.3 pKd
Target used in screen: ABL1(F317I)-phosphorylated
Ligand Sp. Type Action Affinity Units
dasatinib Hs Inhibitor Inhibition 10.4 pKd
bosutinib Hs Inhibitor Inhibition 9.7 pKd
PD-173955 Hs Inhibitor Inhibition 8.3 pKd
AST-487 Hs Inhibitor Inhibition 7.9 pKd
NVP-TAE684 Hs Inhibitor Inhibition 7.8 pKd
nilotinib Hs Inhibitor Inhibition 7.3 pKd
masitinib Hs Inhibitor Inhibition 7.1 pKd
staurosporine Hs Inhibitor Inhibition 6.9 pKd
vandetanib Hs Inhibitor Inhibition 6.8 pKd
foretinib Hs Inhibitor Inhibition 6.6 pKd
Target used in screen: ABL1(F317L)-nonphosphorylated
Ligand Sp. Type Action Affinity Units
dasatinib Hs Inhibitor Inhibition 10.5 pKd
bosutinib Hs Inhibitor Inhibition 10.0 pKd
AST-487 Hs Inhibitor Inhibition 9.1 pKd
imatinib Hs Inhibitor Inhibition 8.6 pKd
PD-173955 Hs Inhibitor Inhibition 8.5 pKd
masitinib Hs Inhibitor Inhibition 8.0 pKd
nilotinib Hs Inhibitor Inhibition 7.9 pKd
foretinib Hs Inhibitor Inhibition 7.7 pKd
NVP-TAE684 Hs Inhibitor Inhibition 7.3 pKd
vandetanib Hs Inhibitor Inhibition 7.1 pKd
Target used in screen: ABL1(F317L)-phosphorylated
Ligand Sp. Type Action Affinity Units
dasatinib Hs Inhibitor Inhibition 10.7 pKd
bosutinib Hs Inhibitor Inhibition 10.5 pKd
PD-173955 Hs Inhibitor Inhibition 8.6 pKd
AST-487 Hs Inhibitor Inhibition 7.9 pKd
nilotinib Hs Inhibitor Inhibition 7.8 pKd
NVP-TAE684 Hs Inhibitor Inhibition 7.7 pKd
vandetanib Hs Inhibitor Inhibition 7.5 pKd
staurosporine Hs Inhibitor Inhibition 7.3 pKd
canertinib Hs Inhibitor Inhibition 7.0 pKd
KW-2449 Hs Inhibitor Inhibition 7.0 pKd
Target used in screen: ABL1(H396P)-nonphosphorylated
Ligand Sp. Type Action Affinity Units
dasatinib Hs Inhibitor Inhibition 10.6 pKd
bosutinib Hs Inhibitor Inhibition 10.2 pKd
PD-173955 Hs Inhibitor Inhibition 9.2 pKd
AST-487 Hs Inhibitor Inhibition 8.6 pKd
tozasertib Hs Inhibitor Inhibition 8.5 pKd
nilotinib Hs Inhibitor Inhibition 8.3 pKd
imatinib Hs Inhibitor Inhibition 8.2 pKd
vandetanib Hs Inhibitor Inhibition 8.0 pKd
foretinib Hs Inhibitor Inhibition 8.0 pKd
masitinib Hs Inhibitor Inhibition 8.0 pKd
Target used in screen: ABL1(H396P)-phosphorylated
Ligand Sp. Type Action Affinity Units
dasatinib Hs Inhibitor Inhibition 10.3 pKd
bosutinib Hs Inhibitor Inhibition 10.2 pKd
PD-173955 Hs Inhibitor Inhibition 8.9 pKd
tozasertib Hs Inhibitor Inhibition 8.5 pKd
vandetanib Hs Inhibitor Inhibition 7.8 pKd
nilotinib Hs Inhibitor Inhibition 7.7 pKd
axitinib Hs Inhibitor Inhibition 7.6 pKd
KW-2449 Hs Inhibitor Inhibition 7.6 pKd
AST-487 Hs Inhibitor Inhibition 7.5 pKd
staurosporine Hs Inhibitor Inhibition 7.4 pKd
Target used in screen: ABL1(M351T)-phosphorylated
Ligand Sp. Type Action Affinity Units
dasatinib Hs Inhibitor Inhibition 10.8 pKd
bosutinib Hs Inhibitor Inhibition 10.4 pKd
PD-173955 Hs Inhibitor Inhibition 9.3 pKd
tozasertib Hs Inhibitor Inhibition 8.3 pKd
nilotinib Hs Inhibitor Inhibition 7.8 pKd
vandetanib Hs Inhibitor Inhibition 7.8 pKd
KW-2449 Hs Inhibitor Inhibition 7.7 pKd
AST-487 Hs Inhibitor Inhibition 7.5 pKd
foretinib Hs Inhibitor Inhibition 7.4 pKd
axitinib Hs Inhibitor Inhibition 7.4 pKd
Target used in screen: ABL1(Q252H)-nonphosphorylated
Ligand Sp. Type Action Affinity Units
dasatinib Hs Inhibitor Inhibition 10.4 pKd
bosutinib Hs Inhibitor Inhibition 10.1 pKd
AST-487 Hs Inhibitor Inhibition 9.0 pKd
PD-173955 Hs Inhibitor Inhibition 8.9 pKd
imatinib Hs Inhibitor Inhibition 8.7 pKd
tozasertib Hs Inhibitor Inhibition 8.4 pKd
foretinib Hs Inhibitor Inhibition 8.4 pKd
masitinib Hs Inhibitor Inhibition 8.2 pKd
nilotinib Hs Inhibitor Inhibition 8.0 pKd
vandetanib Hs Inhibitor Inhibition 7.7 pKd
Target used in screen: ABL1(Q252H)-phosphorylated
Ligand Sp. Type Action Affinity Units
bosutinib Hs Inhibitor Inhibition 10.4 pKd
dasatinib Hs Inhibitor Inhibition 10.2 pKd
PD-173955 Hs Inhibitor Inhibition 9.0 pKd
masitinib Hs Inhibitor Inhibition 8.3 pKd
tozasertib Hs Inhibitor Inhibition 8.0 pKd
staurosporine Hs Inhibitor Inhibition 8.0 pKd
vandetanib Hs Inhibitor Inhibition 7.8 pKd
nilotinib Hs Inhibitor Inhibition 7.7 pKd
KW-2449 Hs Inhibitor Inhibition 7.7 pKd
canertinib Hs Inhibitor Inhibition 7.7 pKd
Target used in screen: ABL1(T315I)-nonphosphorylated
Ligand Sp. Type Action Affinity Units
AST-487 Hs Inhibitor Inhibition 8.6 pKd
axitinib Hs Inhibitor Inhibition 8.4 pKd
staurosporine Hs Inhibitor Inhibition 8.1 pKd
tozasertib Hs Inhibitor Inhibition 8.0 pKd
crizotinib Hs Inhibitor Inhibition 7.9 pKd
KW-2449 Hs Inhibitor Inhibition 7.9 pKd
foretinib Hs Inhibitor Inhibition 7.7 pKd
bosutinib Hs Inhibitor Inhibition 7.7 pKd
NVP-TAE684 Hs Inhibitor Inhibition 7.3 pKd
doramapimod Hs Inhibitor Inhibition 7.2 pKd
Target used in screen: ABL1(T315I)-phosphorylated
Ligand Sp. Type Action Affinity Units
axitinib Hs Inhibitor Inhibition 8.8 pKd
staurosporine Hs Inhibitor Inhibition 8.5 pKd
bosutinib Hs Inhibitor Inhibition 8.4 pKd
NVP-TAE684 Hs Inhibitor Inhibition 8.3 pKd
KW-2449 Hs Inhibitor Inhibition 8.2 pKd
tozasertib Hs Inhibitor Inhibition 8.0 pKd
crizotinib Hs Inhibitor Inhibition 8.0 pKd
cediranib Hs Inhibitor Inhibition 7.7 pKd
vandetanib Hs Inhibitor Inhibition 7.7 pKd
AST-487 Hs Inhibitor Inhibition 7.6 pKd
Target used in screen: ABL1(Y253F)-phosphorylated
Ligand Sp. Type Action Affinity Units
bosutinib Hs Inhibitor Inhibition 10.4 pKd
dasatinib Hs Inhibitor Inhibition 10.2 pKd
PD-173955 Hs Inhibitor Inhibition 9.1 pKd
tozasertib Hs Inhibitor Inhibition 8.1 pKd
vandetanib Hs Inhibitor Inhibition 8.1 pKd
AST-487 Hs Inhibitor Inhibition 8.0 pKd
nilotinib