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Target Report Card

Target Name and Classification

Target ID CHEMBL1862
Preferred Name Tyrosine-protein kinase ABL
Synonyms ABL | ABL1 | Abelson murine leukemia viral oncogene homolog 1 | Abelson tyrosine-protein kinase 1 | JTK7 | Proto-oncogene c-Abl | Tyrosine-protein kinase ABL1 | p150
Organism Homo sapiens
Species Group No
Protein Target Classification
  • enzyme > kinase > protein kinase > tk protein kinase group > tyrosine protein kinase abl family

Target Components

Component Description Relationship Accession
Tyrosine-protein kinase ABL1 SINGLE PROTEIN P00519

Target Relations

ChEMBL ID Pref Name Target Type
CHEMBL3885645 Transcription factor ETV6/Tyrosine-protein kinase ABL1 CHIMERIC PROTEIN
CHEMBL3885630 Ras and Rab interactor 1/Tyrosine-protein kinase ABL1 PROTEIN-PROTEIN INTERACTION
CHEMBL2096618 Bcr/Abl fusion protein CHIMERIC PROTEIN
CHEMBL2111414 Tyrosine-protein kinase ABL PROTEIN FAMILY

Approved Drugs and Clinical Candidates

ChEMBL ID Name Mechanism of Action Max Phase References
CHEMBL288441 BOSUTINIB Tyrosine-protein kinase ABL inhibitor 4 Expert
CHEMBL1421 DASATINIB Tyrosine-protein kinase ABL inhibitor 4 DailyMed
CHEMBL1642 IMATINIB MESYLATE Tyrosine-protein kinase ABL inhibitor 4 DailyMed
CHEMBL1201740 NILOTINIB HYDROCHLORIDE MONOHYDRATE Tyrosine-protein kinase ABL inhibitor 4 DailyMed
CHEMBL1946170 REGORAFENIB Tyrosine-protein kinase ABL inhibitor 4 Expert
CHEMBL2105708 PONATINIB HYDROCHLORIDE Tyrosine-protein kinase ABL inhibitor 4 DailyMed PubMed
CHEMBL217092 SARACATINIB Tyrosine-protein kinase ABL inhibitor 3 PubMed
CHEMBL3545115 ABL-001 Tyrosine-protein kinase ABL inhibitor 3 Other Other
CHEMBL3545413 FLUMATINIB Tyrosine-protein kinase ABL inhibitor 3 PubMed PubMed
CHEMBL206834 BAFETINIB Tyrosine-protein kinase ABL inhibitor 2 PubMed
CHEMBL495727 AT-9283 Tyrosine-protein kinase ABL inhibitor 2 PubMed
CHEMBL1738757 REBASTINIB Tyrosine-protein kinase ABL inhibitor 2 PubMed
CHEMBL3545150 AZM-475271 Tyrosine-protein kinase ABL inhibitor 2 Other
CHEMBL1908397 KW-2449 Tyrosine-protein kinase ABL inhibitor 1 PubMed PubMed
CHEMBL3545085 XL-228 Tyrosine-protein kinase ABL inhibitor 1 DOI Other PubMed
CHEMBL3545177 AZD-0424 Tyrosine-protein kinase ABL inhibitor 1 ClinicalTrials PubMed

Target Associated Bioactivities

Target Associated Assays

Target Ligand Efficiencies

Target Associated Compound Properties

Target Cross References - Gene

Array Express ENSG00000097007
Ensembl ENSG00000097007
GO Cellular Component GO:0005634 (nucleus)
GO:0005654 (nucleoplasm)
GO:0005730 (nucleolus)
GO:0005737 (cytoplasm)
GO:0005739 (mitochondrion)
GO:0005829 (cytosol)
GO:0005856 (cytoskeleton)
GO:0015629 (actin cytoskeleton)
GO:0016020 (membrane)
GO:0016604 (nuclear body)
GO:0030425 (dendrite)
GO:0031234 (extrinsic component of cytoplasmic side of plasma membrane)
GO:0031252 (cell leading edge)
GO:0031965 (nuclear membrane)
GO:0032991 (macromolecular complex)
GO:0043025 (neuronal cell body)
GO:0048471 (perinuclear region of cytoplasm)
GO:0098794 (postsynapse)
GO Molecular Function GO:0000166 (nucleotide binding)
GO:0000287 (magnesium ion binding)
GO:0001784 (phosphotyrosine binding)
GO:0003677 (DNA binding)
GO:0003785 (actin monomer binding)
GO:0004515 (nicotinate-nucleotide adenylyltransferase activity)
GO:0004672 (protein kinase activity)
GO:0004713 (protein tyrosine kinase activity)
GO:0004715 (non-membrane spanning protein tyrosine kinase activity)
GO:0005080 (protein kinase C binding)
GO:0005102 (receptor binding)
GO:0005515 (protein binding)
GO:0005524 (ATP binding)
GO:0008022 (protein C-terminus binding)
GO:0016301 (kinase activity)
GO:0016740 (transferase activity)
GO:0017124 (SH3 domain binding)
GO:0019904 (protein domain specific binding)
GO:0019905 (syntaxin binding)
GO:0030145 (manganese ion binding)
GO:0038191 (neuropilin binding)
GO:0042169 (SH2 domain binding)
GO:0046872 (metal ion binding)
GO:0046875 (ephrin receptor binding)
GO:0051015 (actin filament binding)
GO:0051019 (mitogen-activated protein kinase binding)
GO:0070064 (proline-rich region binding)
GO Biological Process GO:0000278 (mitotic cell cycle)
GO:0001843 (neural tube closure)
GO:0001922 (B-1 B cell homeostasis)
GO:0001934 (positive regulation of protein phosphorylation)
GO:0002322 (B cell proliferation involved in immune response)
GO:0002333 (transitional one stage B cell differentiation)
GO:0006281 (DNA repair)
GO:0006298 (mismatch repair)
GO:0006355 (regulation of transcription, DNA-templated)
GO:0006464 (cellular protein modification process)
GO:0006468 (protein phosphorylation)
GO:0006897 (endocytosis)
GO:0006909 (phagocytosis)
GO:0006914 (autophagy)
GO:0006915 (apoptotic process)
GO:0006974 (cellular response to DNA damage stimulus)
GO:0006975 (DNA damage induced protein phosphorylation)
GO:0006979 (response to oxidative stress)
GO:0007050 (cell cycle arrest)
GO:0007155 (cell adhesion)
GO:0007173 (epidermal growth factor receptor signaling pathway)
GO:0007204 (positive regulation of cytosolic calcium ion concentration)
GO:0007229 (integrin-mediated signaling pathway)
GO:0008630 (intrinsic apoptotic signaling pathway in response to DNA damage)
GO:0009791 (post-embryonic development)
GO:0010506 (regulation of autophagy)
GO:0010595 (positive regulation of endothelial cell migration)
GO:0016310 (phosphorylation)
GO:0018108 (peptidyl-tyrosine phosphorylation)
GO:0021587 (cerebellum morphogenesis)
GO:0022408 (negative regulation of cell-cell adhesion)
GO:0030035 (microspike assembly)
GO:0030036 (actin cytoskeleton organization)
GO:0030100 (regulation of endocytosis)
GO:0030155 (regulation of cell adhesion)
GO:0030182 (neuron differentiation)
GO:0030514 (negative regulation of BMP signaling pathway)
GO:0030516 (regulation of axon extension)
GO:0031113 (regulation of microtubule polymerization)
GO:0032489 (regulation of Cdc42 protein signal transduction)
GO:0032956 (regulation of actin cytoskeleton organization)
GO:0033690 (positive regulation of osteoblast proliferation)
GO:0034446 (substrate adhesion-dependent cell spreading)
GO:0034599 (cellular response to oxidative stress)
GO:0035791 (platelet-derived growth factor receptor-beta signaling pathway)
GO:0038083 (peptidyl-tyrosine autophosphorylation)
GO:0038096 (Fc-gamma receptor signaling pathway involved in phagocytosis)
GO:0038189 (neuropilin signaling pathway)
GO:0042100 (B cell proliferation)
GO:0042127 (regulation of cell proliferation)
GO:0042770 (signal transduction in response to DNA damage)
GO:0043065 (positive regulation of apoptotic process)
GO:0043123 (positive regulation of I-kappaB kinase/NF-kappaB signaling)
GO:0043124 (negative regulation of I-kappaB kinase/NF-kappaB signaling)
GO:0043542 (endothelial cell migration)
GO:0045087 (innate immune response)
GO:0045184 (establishment of protein localization)
GO:0045580 (regulation of T cell differentiation)
GO:0045930 (negative regulation of mitotic cell cycle)
GO:0045931 (positive regulation of mitotic cell cycle)
GO:0046632 (alpha-beta T cell differentiation)
GO:0046777 (protein autophosphorylation)
GO:0048008 (platelet-derived growth factor receptor signaling pathway)
GO:0048536 (spleen development)
GO:0048538 (thymus development)
GO:0048668 (collateral sprouting)
GO:0050731 (positive regulation of peptidyl-tyrosine phosphorylation)
GO:0050798 (activated T cell proliferation)
GO:0050853 (B cell receptor signaling pathway)
GO:0050885 (neuromuscular process controlling balance)
GO:0051149 (positive regulation of muscle cell differentiation)
GO:0051281 (positive regulation of release of sequestered calcium ion into cytosol)
GO:0051353 (positive regulation of oxidoreductase activity)
GO:0051444 (negative regulation of ubiquitin-protein transferase activity)
GO:0051496 (positive regulation of stress fiber assembly)
GO:0051726 (regulation of cell cycle)
GO:0051882 (mitochondrial depolarization)
GO:0051894 (positive regulation of focal adhesion assembly)
GO:0060020 (Bergmann glial cell differentiation)
GO:0060563 (neuroepithelial cell differentiation)
GO:0070301 (cellular response to hydrogen peroxide)
GO:0070373 (negative regulation of ERK1 and ERK2 cascade)
GO:0070374 (positive regulation of ERK1 and ERK2 cascade)
GO:0071222 (cellular response to lipopolysaccharide)
GO:0071901 (negative regulation of protein serine/threonine kinase activity)
GO:0072358 (cardiovascular system development)
GO:0090050 (positive regulation of cell migration involved in sprouting angiogenesis)
GO:0090135 (actin filament branching)
GO:1900026 (positive regulation of substrate adhesion-dependent cell spreading)
GO:1900042 (positive regulation of interleukin-2 secretion)
GO:1900272 (negative regulation of long-term synaptic potentiation)
GO:1900275 (negative regulation of phospholipase C activity)
GO:1901216 (positive regulation of neuron death)
GO:1902036 (regulation of hematopoietic stem cell differentiation)
GO:1902715 (positive regulation of interferon-gamma secretion)
GO:1903053 (regulation of extracellular matrix organization)
GO:1903351 (cellular response to dopamine)
GO:1904528 (positive regulation of microtubule binding)
GO:1904531 (positive regulation of actin filament binding)
GO:1905244 (regulation of modification of synaptic structure)
GO:1905555 (positive regulation blood vessel branching)
GO:1990051 (activation of protein kinase C activity)
GO:2000096 (positive regulation of Wnt signaling pathway, planar cell polarity pathway)
GO:2000145 (regulation of cell motility)
GO:2000249 (regulation of actin cytoskeleton reorganization)
GO:2000251 (positive regulation of actin cytoskeleton reorganization)
GO:2000352 (negative regulation of endothelial cell apoptotic process)
GO:2000772 (regulation of cellular senescence)
GO:2000773 (negative regulation of cellular senescence)
GO:2001020 (regulation of response to DNA damage stimulus)
Wikipedia Abl_gene

Target Cross References - Protein

canSAR P00519
Human Protein Atlas ENSG00000097007
IntAct P00519
Guide to Pharmacology 1923
Open Targets ENSG00000097007
PharmGKB PA24413
Pharos P00519 (Tclin)
Reactome R-HSA-2029482 (Regulation of actin dynamics for phagocytic cup formation.)
R-HSA-375170 (CDO in myogenesis.)
R-HSA-428890 (Role of ABL in ROBO-SLIT signaling.)
R-HSA-5663213 (RHO GTPases Activate WASPs and WAVEs.)
R-HSA-5685938 (HDR through Single Strand Annealing (SSA).)
R-HSA-5693565 (Recruitment and ATM-mediated phosphorylation of repair and signaling proteins at DNA double strand breaks.)
R-HSA-69231 (Cyclin D associated events in G1.)
R-HSA-8939236 (RUNX1 regulates transcription of genes involved in differentiation of HSCs.)
R-HSA-8940973 (RUNX2 regulates osteoblast differentiation.)
R-HSA-983231 (Factors involved in megakaryocyte development and platelet production.)
UniProt A3KFJ3 P00519 Q13869 Q13870 Q16133 Q17R61 Q45F09

Target Cross References - Domain

InterPro IPR000719 (Prot_kinase_dom.)
IPR000980 (SH2.)
IPR001245 (Ser-Thr/Tyr_kinase_cat_dom.)
IPR001452 (SH3_domain.)
IPR008266 (Tyr_kinase_AS.)
IPR011009 (Kinase-like_dom_sf.)
IPR015015 (F-actin_binding.)
IPR017441 (Protein_kinase_ATP_BS.)
IPR020635 (Tyr_kinase_cat_dom.)
IPR033221 (ABL1.)
IPR035837 (ABL_SH2.)
IPR036028 (SH3-like_dom_sf.)
IPR036860 (SH2_dom_sf.)
Pfam PF00017 (SH2)
PF00018 (SH3_1)
PF07714 (Pkinase_Tyr)
PF08919 (F_actin_bind)

Target Cross References - Structure

PDBe 1BBZ 1OPL 2ABL 2E2B 2F4J 2FO0 2G1T 2G2F 2G2H 2G2I 2GQG 2HIW 2HYY 2HZ0 2HZ4 2HZI 2O88 2V7A 3CS9 3EG0 3EG1 3EG2 3EG3 3EGU More...
CREDO 1BBZ 1OPL 2ABL 2E2B 2F4J 2FO0 2G1T 2G2F 2G2H 2G2I 2GQG 2HIW 2HYY 2HZ0 2HZ4 2HZI 2O88 2V7A 3CS9 3EG0 3EG1 3EG2 3EG3 3EGU More...