DGIdb - ABL1 Gene Record

ABL1 25 Druggable GenomeClinically ActionableDrug Resistance

Alternate Names:

25
ABL PROTO-ONCOGENE 1, NON-RECEPTOR TYROSINE KINASE
ABL1
ABL
CHDSKM
JTK7
bcr/abl
c-ABL
c-ABL1
p150
v-abl
189980
76
ENSG00000097007
OTTHUMG00000020813
P00519
ABL1_HUMAN
Abelson tyrosine-protein kinase 1
Proto-oncogene c-Abl
Abelson murine leukemia viral oncogene homolog 1
Tyrosine-protein kinase ABL1
PROTO-ONCOGENE TYROSINE-PROTEIN KINASE ABL1 (EC 2.7.1.112) (P150) (C- ABL). [SOURCE:UNIPROT/SWISSPROT;ACC:P00519]
BE0000014
PA24413
4
1923
NP_005148
NM_005157
T63505

Gene Info:

Human Readable Name	DRUGGABLE GENOME
Target Class	Enzymes
Target Subclass	EC:2.7.10.2
Uniprot Status	Swiss-Prot
Interpro Short Name	Ser-Thr/Tyr_kinase_cat_dom
Human Readable Name	KINASE
Interpro Name	Serine-threonine/tyrosine-protein kinase catalytic domain
Interpro Acc	IPR001245
Uniprot Evidence	1: Evidence at protein level
Interpro Type	Domain
Target Subclass	2.7.10.2
Target Main Class	Enzymes
Initial Gene Query	ABL
Counted Citations from 1950-2000	7889
GuideToPharmacology Gene Category Name	Abl family
GuideToPharmacology Gene Category ID	553
Gene Biotype	PROTEIN_CODING

(25 More Sources)

Gene Categories: Category Details

KINASE
TYROSINE KINASE
DRUG RESISTANCE
DRUGGABLE GENOME
CLINICALLY ACTIONABLE
ENZYME

Publications:

Deora et al., Down-modulation of P210bcr/abl induces apoptosis/differentiation in K562 leukemic blast cells., Tumori
Al-Ali et al., 2004, High incidence of BCR-ABL kinase domain mutations and absence of mutations of the PDGFR and KIT activation loops in CML patients with secondary resistance to imatinib., Hematol. J.
An et al., 2010, BCR-ABL tyrosine kinase inhibitors in the treatment of Philadelphia chromosome positive chronic myeloid leukemia: a review., Leuk. Res.
O'Hare et al., 2004, Inhibition of wild-type and mutant Bcr-Abl by AP23464, a potent ATP-based oncogenic protein kinase inhibitor: implications for CML., Blood
Testoni et al., 2016, Somatically mutated ABL1 is an actionable and essential NSCLC survival gene., EMBO Mol Med
Chahardouli et al., 2013, Detection of BCR-ABL kinase domain mutations in patients with chronic myeloid leukemia on imatinib., Hematology
Burgess MR et al., 2005, Comparative analysis of two clinically active BCR-ABL kinase inhibitors reveals the role of conformation-specific binding in resistance., Proc Natl Acad Sci U S A
Müller MC et al., 2009, Dasatinib treatment of chronic-phase chronic myeloid leukemia: analysis of responses according to preexisting BCR-ABL mutations., Blood
von Bubnoff et al., 2002, BCR-ABL gene mutations in relation to clinical resistance of Philadelphia-chromosome-positive leukaemia to STI571: a prospective study., Lancet
Qin et al., 2011, Characteristics of BCR-ABL kinase domain point mutations in Chinese imatinib-resistant chronic myeloid leukemia patients., Ann. Hematol.
Talpaz M et al., 2006, Dasatinib in imatinib-resistant Philadelphia chromosome-positive leukemias., N Engl J Med
Tomita O et al., 2014, Sensitivity of SNX2-ABL1 toward tyrosine kinase inhibitors distinct from that of BCR-ABL1., Leuk Res
Doi et al., 2009, High-resolution melting analysis for a reliable and two-step scanning of mutations in the tyrosine kinase domain of the chimerical bcr-abl gene., Int. J. Hematol.
Deguchi Y et al., 2008, Comparison of imatinib, dasatinib, nilotinib and INNO-406 in imatinib-resistant cell lines., Leuk Res
Pemovska T et al., 2015, Axitinib effectively inhibits BCR-ABL1(T315I) with a distinct binding conformation., Nature
Sharma et al., 2010, Mutations in ABL kinase domain are associated with inferior progression-free survival., Leuk. Lymphoma
Piccaluga et al., 2007, Tyrosine kinase inhibitors for the treatment of Philadelphia chromosome-positive adult acute lymphoblastic leukemia., Cancer
Roberts et al., 2014, Targetable kinase-activating lesions in Ph-like acute lymphoblastic leukemia., N. Engl. J. Med.
Sorel et al., 2004, Evidence of ABL-kinase domain mutations in highly purified primitive stem cell populations of patients with chronic myelogenous leukemia., Biochem. Biophys. Res. Commun.
Strhakova et al., 2011, Use of direct sequencing for detection of mutations in the BCR-ABL kinase domain in Slovak patients with chronic myeloid leukemia., Neoplasma
Jabbour et al., 2008, Characteristics and outcome of chronic myeloid leukemia patients with F317L BCR-ABL kinase domain mutation after therapy with tyrosine kinase inhibitors., Blood
Branford et al., 2002, High frequency of point mutations clustered within the adenosine triphosphate-binding region of BCR/ABL in patients with chronic myeloid leukemia or Ph-positive acute lymphoblastic leukemia who develop imatinib (STI571) resistance., Blood
Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
Elias et al., 2014, BCR-ABL kinase domain mutations, including 2 novel mutations in imatinib resistant Malaysian chronic myeloid leukemia patients-Frequency and clinical outcome., Leuk. Res.
Jones et al., 2008, Kinase domain point mutations in Philadelphia chromosome-positive acute lymphoblastic leukemia emerge after therapy with BCR-ABL kinase inhibitors., Cancer
MacConaill et al., 2014, Prospective enterprise-level molecular genotyping of a cohort of cancer patients., J Mol Diagn
von Bubnoff et al., 2003, Inhibition of wild-type and mutant Bcr-Abl by pyrido-pyrimidine-type small molecule kinase inhibitors., Cancer Res.
Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov
Soverini et al., 2011, BCR-ABL kinase domain mutation analysis in chronic myeloid leukemia patients treated with tyrosine kinase inhibitors: recommendations from an expert panel on behalf of European LeukemiaNet., Blood
Eide et al., 2011, The ABL switch control inhibitor DCC-2036 is active against the chronic myeloid leukemia mutant BCR-ABLT315I and exhibits a narrow resistance profile., Cancer Res.
Hughes et al., 2009, Impact of baseline BCR-ABL mutations on response to nilotinib in patients with chronic myeloid leukemia in chronic phase., J. Clin. Oncol.
Bradeen HA et al., 2006, Comparison of imatinib mesylate, dasatinib (BMS-354825), and nilotinib (AMN107) in an N-ethyl-N-nitrosourea (ENU)-based mutagenesis screen: high efficacy of drug combinations., Blood
Hochhaus et al., 2002, Molecular and chromosomal mechanisms of resistance to imatinib (STI571) therapy., Leukemia
Kantarjian et al., 2007, Nilotinib (formerly AMN107), a highly selective BCR-ABL tyrosine kinase inhibitor, is effective in patients with Philadelphia chromosome-positive chronic myelogenous leukemia in chronic phase following imatinib resistance and intolerance., Blood
Maekawa et al., 2007, The Bcr-Abl tyrosine kinase inhibitor imatinib and promising new agents against Philadelphia chromosome-positive leukemias., Int. J. Clin. Oncol.
Redaelli et al., 2009, Activity of bosutinib, dasatinib, and nilotinib against 18 imatinib-resistant BCR/ABL mutants., J. Clin. Oncol.
Weisberg et al., 2006, AMN107 (nilotinib): a novel and selective inhibitor of BCR-ABL., Br. J. Cancer
Branford et al., 2003, Detection of BCR-ABL mutations in patients with CML treated with imatinib is virtually always accompanied by clinical resistance, and mutations in the ATP phosphate-binding loop (P-loop) are associated with a poor prognosis., Blood
Soverini et al., 2006, Presence or the emergence of a F317L BCR-ABL mutation may be associated with resistance to dasatinib in Philadelphia chromosome-positive leukemia., J. Clin. Oncol.
Cang et al., 2008, P-loop mutations and novel therapeutic approaches for imatinib failures in chronic myeloid leukemia., J Hematol Oncol
Zick et al., 2017, Treatment inferred from mutations identified using massive parallel sequencing leads to clinical benefit in some heavily pretreated cancer patients., Medicine (Baltimore)
Oyekunle et al., 2011, F317L BCR-ABL1 kinase domain mutation associated with a sustained major molecular response in a CML patient on dasatinib., Leuk. Res.
Eskazan et al., 2011, Chronic myeloid leukemia patients with F317L BCR-ABL kinase domain mutation are resistant to dasatinib: is that true for all the patients?, Leuk. Res.
Rosti et al., 2009, Nilotinib for the frontline treatment of Ph(+) chronic myeloid leukemia., Blood
Swords et al., 2009, Nilotinib: optimal therapy for patients with chronic myeloid leukemia and resistance or intolerance to imatinib., Drug Des Devel Ther
Manrique Arechavaleta et al., 2011, Rapid and sensitive allele-specific (AS)-RT-PCR assay for detection of T315I mutation in chronic myeloid leukemia patients treated with tyrosine-kinase inhibitors., Clin. Exp. Med.
Hofmann et al., 2002, Ph(+) acute lymphoblastic leukemia resistant to the tyrosine kinase inhibitor STI571 has a unique BCR-ABL gene mutation., Blood
Gorre et al., 2001, Clinical resistance to STI-571 cancer therapy caused by BCR-ABL gene mutation or amplification., Science
Minami et al., 2010, Expanded distribution of the T315I mutation among hematopoietic stem cells and progenitors in a chronic myeloid leukemia patient during imatinib treatment., Int. J. Hematol.
Giles et al., 2013, MK-0457, an Aurora kinase and BCR-ABL inhibitor, is active in patients with BCR-ABL T315I leukemia., Leukemia
Yin et al., 2012, Rapid quantitative detection of the T315I mutation in patients with chronic myelogenous leukemia., Diagn. Mol. Pathol.
Cortes et al., 2012, Ponatinib in refractory Philadelphia chromosome-positive leukemias., N. Engl. J. Med.
Ferri et al., 2013, Early detection and quantification of mutations in the tyrosine kinase domain of chimerical BCR-ABL1 gene combining high-resolution melting analysis and mutant-allele specific quantitative polymerase chain reaction., Leuk. Lymphoma
Paquette et al., 2011, Frequent EVI1 translocations in myeloid blast crisis CML that evolves through tyrosine kinase inhibitors., Cancer Genet
Roche-Lestienne et al., 2002, Several types of mutations of the Abl gene can be found in chronic myeloid leukemia patients resistant to STI571, and they can pre-exist to the onset of treatment., Blood
Tanneeru et al., 2013, Ponatinib is a pan-BCR-ABL kinase inhibitor: MD simulations and SIE study., PLoS ONE
Chahardouli et al., 2013, Evaluation of T315I mutation frequency in chronic myeloid leukemia patients after imatinib resistance., Hematology
Huang et al., 2010, Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including the T315I gatekeeper mutant., J. Med. Chem.
Elias et al., 2012, Contribution of BCR-ABL kinase domain mutations to imatinib mesylate resistance in Philadelphia chromosome positive Malaysian chronic myeloid leukemia patients., Hematol Rep
Miller et al., 2014, Resistant mutations in CML and Ph(+)ALL - role of ponatinib., Biologics
Iqbal et al., 2013, Sensitive detection of pre-existing BCR-ABL kinase domain mutations in CD34+ cells of newly diagnosed chronic-phase chronic myeloid leukemia patients is associated with imatinib resistance: implications in the post-imatinib era., PLoS ONE
Yamamoto et al., 2004, The two major imatinib resistance mutations E255K and T315I enhance the activity of BCR/ABL fusion kinase., Biochem. Biophys. Res. Commun.
Soverini et al., 2011, Low-level Bcr-Abl mutations are very rare in chronic myeloid leukemia patients who are in major molecular response on first-line nilotinib., Leuk. Res.
Haberler et al., 2006, Immunohistochemical analysis of platelet-derived growth factor receptor-alpha, -beta, c-kit, c-abl, and arg proteins in glioblastoma: possible implications for patient selection for imatinib mesylate therapy., J. Neurooncol.
Perwein T et al., 2016, Imatinib-induced long-term remission in a relapsed RCSD1-ABL1-positive acute lymphoblastic leukemia., Haematologica
O'Hare et al., 2005, In vitro activity of Bcr-Abl inhibitors AMN107 and BMS-354825 against clinically relevant imatinib-resistant Abl kinase domain mutants., Cancer Res.
Dewar et al., 2005, Inhibition of c-fms by imatinib: expanding the spectrum of treatment., Cell Cycle
Ivan et al., 2006, Analysis of protein tyrosine kinases expression in the melanoma metastases of patients treated with Imatinib Mesylate (STI571, Gleevec)., J. Cutan. Pathol.
Page BD et al., 2012, Small molecule STAT5-SH2 domain inhibitors exhibit potent antileukemia activity., J Med Chem
Khoury HJ et al., 2012, Bosutinib is active in chronic phase chronic myeloid leukemia after imatinib and dasatinib and/or nilotinib therapy failure., Blood
Hoerth et al., 2004, Involvment of c-Abl in the radiation-induced inhibition of myoblast differentiation., Int. J. Radiat. Biol.
Agirre et al., 2005, Coexistence of different clonal populations harboring the b3a2 (p210) and e1a2 (p190) BCR-ABL1 fusion transcripts in chronic myelogenous leukemia resistant to imatinib., Cancer Genet. Cytogenet.
Brueggemeier et al., Protein-acrylamide copolymer hydrogels for array-based detection of tyrosine kinase activity from cell lysates., Biomacromolecules
Nimmanapalli et al., 2002, Novel targeted therapies for Bcr-Abl positive acute leukemias: beyond STI571., Oncogene
Mojzych M et al., 2014, Synthesis and kinase inhibitory activity of new sulfonamide derivatives of pyrazolo[4,3-e][1,2,4]triazines., Eur J Med Chem
Kim et al., 2014, Efficacy and safety of radotinib in chronic phase chronic myeloid leukemia patients with resistance or intolerance to BCR-ABL1 tyrosine kinase inhibitors., Haematologica
Adrián FJ et al., 2006, Allosteric inhibitors of Bcr-abl-dependent cell proliferation., Nat Chem Biol
Nehmé et al., 1999, Induction of JNK and c-Abl signalling by cisplatin and oxaliplatin in mismatch repair-proficient and -deficient cells., Br. J. Cancer
Hudkins RL et al., 2012, Synthesis and biological profile of the pan-vascular endothelial growth factor receptor/tyrosine kinase with immunoglobulin and epidermal growth factor-like homology domains 2 (VEGF-R/TIE-2) inhibitor 11-(2-methylpropyl)-12,13-dihydro-2-methyl-8-(pyrimidin-2-ylamino)-4H-indazolo[5,4-a]pyrrolo[3,4-c]carbazol-4-one (CEP-11981): a novel oncology therapeutic agent., J Med Chem
Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov
Dorey et al., 1999, Regulation of human c-Abl tyrosine kinase activity in Xenopus oocytes and acceleration of progesterone-induced G2/M transition by oncogenic forms., Biol. Chem.
Nishimaki et al., 1996, Inhibitory effect of a nucleoside analog, acyclovir, on leukemia cells., Leuk. Res.
Chapman et al., 1994, The suppression of drug-induced apoptosis by activation of v-ABL protein tyrosine kinase., Cancer Res.
Haupt et al., 2006, Celecoxib can induce cell death independently of cyclooxygenase-2, p53, Mdm2, c-Abl and reactive oxygen species., Anticancer Drugs
del Senno et al., 1986, Methylation and expression of c-myc and c-abl oncogenes in human leukemic K562 cells before and after treatment with 5-azacytidine., Cancer Detect. Prev.
Berman et al., 2000, The Protein Data Bank., Nucleic Acids Res.
Rolf MG et al., 2015, In vitro pharmacological profiling of R406 identifies molecular targets underlying the clinical effects of fostamatinib., Pharmacol Res Perspect
Ceccon M et al., 2013, Crizotinib-resistant NPM-ALK mutants confer differential sensitivity to unrelated Alk inhibitors., Mol Cancer Res
Markham A, 2017, Brigatinib: First Global Approval., Drugs

ASCIMINIB ABL1

Interaction Score: 2.27

Interaction Types & Directionality:

allosteric modulator

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Tyrosine-protein kinase ABL inhibitor

Direct Interaction yes

Details of the Assay for Interaction Two assays used: a radiometric filter-binding assay and microfluidic mobility shift technology (Caliper assay).

PMIDs:
None found

Sources:
OncoKB GuideToPharmacology ChemblInteractions

NILOTINIB ABL1

Interaction Score: 2.1

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name nilotinib , AMN-107,Tasigna

Novel drug target Established target

Variant Effect gain-of-function

PMIDs:
17715389 20537386 17929114 19075254 23676790 16721371 12623848 18191450 25686603 20367437 17114651 18828913 28514312 21895409 21489624 11964322 25157968 21605905 19822896 21562040 19652056 16772610 19920925

Sources:
TEND OncoKB FDA PharmGKB DoCM JAX-CKB TdgClinicalTrial CIViC DrugBank COSMIC MyCancerGenome GuideToPharmacology CGI
CHEMBL327127 ABL1

Interaction Score: 1.51

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
10592235

Sources:
DrugBank
RADOTINIB ABL1

Interaction Score: 1.51

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

PMIDs:
24705186

Sources:
DrugBank
PONATINIB ABL1

Interaction Score: 1.36

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Drug family BCR-ABL inhibitor 3rd gen&Pan-TK inhibitor

Alteration ABL1:T315I

Alteration ABL1__BCR

PMIDs:
20512393 14745431 20537386 11861307 15256422 11423618 20963643 22772060 22306673 23676790 11853795 23190221 22870928 20697894 21872826 12623848 19466505 12130516 20367437 17114651 18828913 24236021 15381060 23540562 21895409 20513156 21489624 23355941 11964322 25349473 24456693 18615627 25157968 23409026 14559829 21605905 21562040 21505103 19652056 15194504 21762985 12399961

Sources:
DTC OncoKB FDA PharmGKB DoCM TdgClinicalTrial CIViC TTD DrugBank MyCancerGenome GuideToPharmacology CGI
BOSUTINIB ABL1

Interaction Score: 1.15

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Variant Effect gain-of-function

Pathway activation

Clinical Status NCCN guidelines

PMIDs:
14745431 15256422 23676790 11853795 20697894 12623848 19466505 20367437 17114651 18828913 15381060 21895409 21489624 11964322 24456693 18615627 25157968 14559829 21605905 21562040 21505103 19652056 12399961

Sources:
OncoKB FDA PharmGKB DoCM TdgClinicalTrial TTD DrugBank COSMIC MyCancerGenome GuideToPharmacology ChemblInteractions CGI
BAFETINIB ABL1

Interaction Score: 0.95

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Tyrosine-protein kinase ABL inhibitor

Direct Interaction yes

Specific Action of the Ligand Inhibition

PMIDs:
18191450

Sources:
CIViC MyCancerGenome GuideToPharmacology ChemblInteractions
PF-114 ABL1

Interaction Score: 0.76

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction Inhibition of native ABL kinase activity.

Specific Action of the Ligand Inhibition

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
NILOTINIB HYDROCHLORIDE MONOHYDRATE ABL1

Interaction Score: 0.76

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Tyrosine-protein kinase ABL inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
FLUMATINIB ABL1

Interaction Score: 0.76

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
TTD GuideToPharmacology ChemblInteractions
CHEMBL483847 ABL1

Interaction Score: 0.5

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16415863

Sources:
DTC
REBASTINIB ABL1

Interaction Score: 0.45

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Tyrosine-protein kinase ABL inhibitor

Direct Interaction yes

Specific Action of the Ligand Inhibition

PMIDs:
None found

Sources:
TTD GuideToPharmacology ChemblInteractions
KW-2449 ABL1

Interaction Score: 0.45

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Tyrosine-protein kinase ABL inhibitor

Direct Interaction yes

Specific Action of the Ligand Inhibition

PMIDs:
None found

Sources:
TTD GuideToPharmacology ChemblInteractions
DASATINIB ABL1

Interaction Score: 0.44

Interaction Types & Directionality:

multitarget

inhibitor (inhibitory)

Interaction Info:

combination therapy [Nilotinib,Dasatinib]

Drug family [BCR-ABL inhibitor 2nd gen]

Alteration ABL1:T315I

PMIDs:
14745431 20537386 15256422 26758680 23676790 15705718 19779040 11853795 20697894 16775234 24367893 19466505 18191450 25686603 20367437 17701954 25207766 15381060 21895409 18818391 11964322 11752352 24456693 18615627 25157968 14559829 17016423 21562040 21505103 19652056 16772610 12399961

Sources:
TEND OncoKB FDA PharmGKB DoCM JAX-CKB TdgClinicalTrial CIViC DrugBank COSMIC MyCancerGenome GuideToPharmacology ChemblInteractions CGI
IMATINIB ABL1

Interaction Score: 0.4

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Fusion protein BCR:ABL1

Trial Name imatinib mesylate, STI 571,Gleevec, Glivec

Novel drug target Established target

PMIDs:
20537386 26758680 16205964 19075254 27125982 15930265 15917650 16775234 24367893 12623848 16630177 18191450 25686603 25207766 22148584 22371878 15799618 15949566 16153117 12476305 15194504 24681986

Sources:
NCI TEND DTC OncoKB FDA PharmGKB JAX-CKB TdgClinicalTrial CIViC DrugBank COSMIC MyCancerGenome GuideToPharmacology CGI
PONATINIB HYDROCHLORIDE ABL1

Interaction Score: 0.38

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Tyrosine-protein kinase ABL inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
AZD-0424 ABL1

Interaction Score: 0.38

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Tyrosine-protein kinase ABL inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
AZM-475271 ABL1

Interaction Score: 0.38

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Tyrosine-protein kinase ABL inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
ACYCLOVIR ABL1

Interaction Score: 0.3

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
8683981

Sources:
NCI
CHEMBL219557 ABL1

Interaction Score: 0.25

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
BRIGATINIB ABL1

Interaction Score: 0.23

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
23239810 28597393

Sources:
DrugBank
AXITINIB ABL1

Interaction Score: 0.22

Interaction Types & Directionality:

n/a

Interaction Info:

Alteration ABL1:T315I

Drug family VEGFR inhibitor

PMIDs:
25686603

Sources:
PharmGKB CIViC CGI
BLINATUMOMAB ABL1

Interaction Score: 0.22

Interaction Types & Directionality:

n/a

Interaction Info:

Fusion protein BCR:ABL1

PMIDs:
None found

Sources:
FDA PharmGKB
OMACETAXINE MEPESUCCINATE ABL1

Interaction Score: 0.19

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
XL-228 ABL1

Interaction Score: 0.18

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name XL228

Novel drug target Established target

Mechanism of Interaction Tyrosine-protein kinase ABL inhibitor

PMIDs:
None found

Sources:
TdgClinicalTrial DrugBank MyCancerGenome ChemblInteractions
SARACATINIB ABL1

Interaction Score: 0.17

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Tyrosine-protein kinase ABL inhibitor

Direct Interaction yes

Specific Action of the Ligand Inhibition

PMIDs:
None found

Sources:
TTD GuideToPharmacology ChemblInteractions
AT-9283 ABL1

Interaction Score: 0.12

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Tyrosine-protein kinase ABL inhibitor

PMIDs:
None found

Sources:
MyCancerGenome ChemblInteractions
HYDROXYUREA ABL1

Interaction Score: 0.11

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
7923130

Sources:
NCI
PEXMETINIB ABL1

Interaction Score: 0.1

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
TdgClinicalTrial GuideToPharmacology
BUSULFAN ABL1

Interaction Score: 0.09

Interaction Types & Directionality:

n/a

Interaction Info:

Fusion protein BCR:ABL1

PMIDs:
None found

Sources:
FDA PharmGKB
CEP-11981 ABL1

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22148921

Sources:
DTC
MELPHALAN ABL1

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
7923130

Sources:
NCI
ADENOSINE TRIPHOSPHATE ABL1

Interaction Score: 0.08

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
16415863 11752352 17139284 17016423

Sources:
DTC DrugBank
IMATINIB MESYLATE ABL1

Interaction Score: 0.08

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Tyrosine-protein kinase ABL inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
AZAKENPAULLONE ABL1

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
MYRISTIC ACID ABL1

Interaction Score: 0.07

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
10592235

Sources:
DrugBank
MASITINIB ABL1

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name masitinib, AB1010

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial
REGORAFENIB ABL1

Interaction Score: 0.05

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Tyrosine-protein kinase ABL inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
DrugBank ChemblInteractions
VENETOCLAX ABL1

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Dasatinib;Venetoclax

Drug family BCR-ABL inhibitor 2nd gen;BCL2 inhibitor

Alteration ABL1__BCR

PMIDs:
None found

Sources:
CGI
CABOZANTINIB ABL1

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

Drug family Pan-kinase inhibitor

Alteration ABL1:V299L

PMIDs:
None found

Sources:
CGI
AZACITIDINE ABL1

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
2425967

Sources:
NCI
OXALIPLATIN ABL1

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
10098743

Sources:
NCI
CRIZOTINIB ABL1

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

Drug family ALK inhibitor

Alteration ABL1:V299L

PMIDs:
None found

Sources:
CGI
ENMD-2076 ABL1

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name ENMD-2076

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial
MLN-8054 ABL1

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
VANDETANIB ABL1

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

Drug family Pan-TK inhibitor

Alteration ABL1:V299L

PMIDs:
None found

Sources:
DTC CGI
CHEMBL406845 ABL1

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ADAVOSERTIB ABL1

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
VINCRISTINE ABL1

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

Fusion protein BCR:ABL1

PMIDs:
None found

Sources:
FDA PharmGKB
GENISTEIN ABL1

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
9349317

Sources:
NCI
CHEMBL546797 ABL1

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
CELECOXIB ABL1

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16917206

Sources:
NCI
AST-487 ABL1

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
PROGESTERONE ABL1

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
10195429

Sources:
NCI
ALISERTIB ABL1

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
OSI-632 ABL1

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
CHEMBL379975 ABL1

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
TRAMETINIB ABL1

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Trametinib;Imatinib

Drug family MEK inhibitor;BCR-ABL inhibitor 1st gen&KIT inhibitor

Alteration PRKCH:amp;ABL1__BCR

PMIDs:
None found

Sources:
CGI
PAZOPANIB ABL1

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
KENPAULLONE ABL1

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
CEDIRANIB ABL1

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ALSTERPAULLONE ABL1

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
JNJ-7706621 ABL1

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
PD-0166285 ABL1

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
QUERCETIN ABL1

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
9349317

Sources:
NCI
ERLOTINIB ABL1

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
CENISERTIB ABL1

Interaction Score: 0.01

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
DTC MyCancerGenome
ENTRECTINIB ABL1

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
TOZASERTIB ABL1

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
SORAFENIB ABL1

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DOVITINIB ABL1

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
CYC-116 ABL1

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
TAE-684 ABL1

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ILORASERTIB ABL1

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
FOSTAMATINIB ABL1

Interaction Score: 0.01

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
26516587

Sources:
DrugBank

Ensembl: ENSG00000097007
- Version: 101_38
Alternate Names:

ABL1 Ensembl Gene Name

Gene Info:

Gene Biotype PROTEIN_CODING

Publications:
TEND: P00519
- Version: 01-August-2011
Alternate Names:

ABL1_HUMAN Uniprot Id

P00519 Uniprot Accession

ENSG00000097007 Ensembl Gene Id

Gene Info:

Target Subclass 2.7.10.2

Target Main Class Enzymes

Publications:
BaderLabGenes: ABL1
- Version: February-2014
Alternate Names:

25 Entrez Gene ID

Gene Info:

Initial Gene Query ABL

Counted Citations from 1950-2000 7889

Gene Categories:

KINASE

Publications:
RussLampel: ENSG00000097007
- Version: 26-July-2011
Alternate Names:

ENSG00000097007 Ensembl Gene Id

ABL1 Display Id

PROTO-ONCOGENE TYROSINE-PROTEIN KINASE ABL1 (EC 2.7.1.112) (P150) (C- ABL). [SOURCE:UNIPROT/SWISSPROT;ACC:P00519] Description

Gene Info:

Human Readable Name DRUGGABLE GENOME

Gene Categories:

DRUGGABLE GENOME

Publications:
HopkinsGroom: P00519
- Version: 11-September-2012
Alternate Names:

TYROSINE-PROTEIN KINASE ABL1 Uniprot Protein Name

ENSG00000097007 Ensembl Gene Id

25 Entrez Gene Id

Gene Info:

Uniprot Status Swiss-Prot

Interpro Short Name Ser-Thr/Tyr_kinase_cat_dom

Human Readable Name KINASE

Gene Categories:

KINASE, DRUGGABLE GENOME

Publications:
TdgClinicalTrial: P00519
- Version: January-2014
Alternate Names:

ABL1 Gene Symbol

Gene Info:

Target Class Enzymes

Target Subclass EC:2.7.10.2

Publications:
GuideToPharmacology: 25
- Version: 29-September-2020
Alternate Names:

76 HUGO Gene ID

76 HUGO Gene Symbol

ABL proto-oncogene 1, non-receptor tyrosine kinase HUGO Gene Name

Gene Info:

GuideToPharmacology Gene Category Name Abl family

GuideToPharmacology Gene Category ID 553

Gene Categories:

ENZYME

Publications:

JAX-CKB: ABL1

Version: 27-September-2017

Alternate Names:

25 CKB Entrez Id

ABL1 CKB Gene Synonym

ABL CKB Gene Synonym

Gene Info:

Publications:

Zick et al., 2017, Treatment inferred from mutations identified using massive parallel sequencing leads to clinical benefit in some heavily pretreated cancer patients., Medicine (Baltimore)

Testoni et al., 2016, Somatically mutated ABL1 is an actionable and essential NSCLC survival gene., EMBO Mol Med

PharmGKB: ABL1
- Version: 18-August-2020
Alternate Names:

PA24413 PharmGKB ID

Gene Info:

Publications:

Pemovska T et al., 2015, Axitinib effectively inhibits BCR-ABL1(T315I) with a distinct binding conformation., Nature

CIViC: ABL1

Version: 14-September-2020

Alternate Names:

25 Entrez Gene ID

4 CIViC Gene ID

Gene Info:

Gene Categories:

DRUG RESISTANCE, CLINICALLY ACTIONABLE

Publications:

Chen Y et al., 2009, Inhibitory effects of omacetaxine on leukemic stem cells and BCR-ABL-induced chronic myeloid leukemia and acute lymphoblastic leukemia in mice., Leukemia

Cortes J et al., 2012, Phase 2 study of subcutaneous omacetaxine mepesuccinate after TKI failure in patients with chronic-phase CML with T315I mutation., Blood

Testoni et al., 2016, Somatically mutated ABL1 is an actionable and essential NSCLC survival gene., EMBO Mol Med

DrugBank: BE0000014

Version: 5.1.7

Alternate Names:

ABL1 DrugBank Gene Name

P00519 UniProt Accession

25 Entrez Gene Id

Gene Info:

Publications:

Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.

Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov

Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov

NCI: ABL1

Version: 14-September-2017

Alternate Names:

Gene Info:

Publications:

Deora et al., Down-modulation of P210bcr/abl induces apoptosis/differentiation in K562 leukemic blast cells., Tumori

Chapman et al., 1994, The suppression of drug-induced apoptosis by activation of v-ABL protein tyrosine kinase., Cancer Res.

Haupt et al., 2006, Celecoxib can induce cell death independently of cyclooxygenase-2, p53, Mdm2, c-Abl and reactive oxygen species., Anticancer Drugs

DoCM: ABL1

Version: 27-September-2017

Alternate Names:

Gene Info:

Publications:

Chahardouli et al., 2013, Detection of BCR-ABL kinase domain mutations in patients with chronic myeloid leukemia on imatinib., Hematology

Branford et al., 2003, Detection of BCR-ABL mutations in patients with CML treated with imatinib is virtually always accompanied by clinical resistance, and mutations in the ATP phosphate-binding loop (P-loop) are associated with a poor prognosis., Blood

Sharma et al., 2010, Mutations in ABL kinase domain are associated with inferior progression-free survival., Leuk. Lymphoma

DTC: ABL1

Version: 02-September-2020

Alternate Names:

Gene Info:

Publications:

Adrián FJ et al., 2006, Allosteric inhibitors of Bcr-abl-dependent cell proliferation., Nat Chem Biol

Page BD et al., 2012, Small molecule STAT5-SH2 domain inhibitors exhibit potent antileukemia activity., J Med Chem

Mojzych M et al., 2014, Synthesis and kinase inhibitory activity of new sulfonamide derivatives of pyrazolo[4,3-e][1,2,4]triazines., Eur J Med Chem

HingoraniCasas: ENSG00000097007
- Version: 31-May-2017
Alternate Names:

ENSG00000097007 Gene Symbol

ABL1 Ensembl Id

Gene Info:

Gene Categories:

DRUGGABLE GENOME

Publications:
MyCancerGenome: ABL1
- Version: 20-Jun-2017
Alternate Names:

25 Entrez Gene Id

ABL1 MyCancerGenome Gene Symbol

ABL MyCancerGenome Reported Gene Name

Gene Info:

Publications:
ChemblInteractions: ABL
- Version: chembl_23
Alternate Names:

JTK7 GENE_SYMBOL

ABL1 GENE_SYMBOL

Tyrosine-protein kinase ABL1 UNIPROT

Gene Info:

Publications:
OncoKB: ABL1
- Version: 23-July-2020
Alternate Names:

p150 OncoKB Gene Synonym

25 OncoKB Entrez Id

v-abl OncoKB Gene Synonym

Gene Info:

Publications:
Pharos: ABL1
- Version: 03-September-2020
Alternate Names:

Tyrosine-protein kinase ABL1 Gene Name

P00519 UniProt ID

Gene Info:

Gene Categories:

KINASE

Publications:
GO: ABL1
- Version: 05-September-2020
Alternate Names:

ABL GO Gene Synonym

JTK7 GO Gene Synonym

Gene Info:

Gene Categories:

KINASE, TYROSINE KINASE

Publications:
Tempus: ABL1
- Version: 11-November-2018
Alternate Names:

ABL1 Gene Symbol

Gene Info:

Gene Categories:

CLINICALLY ACTIONABLE

Publications:
dGene: ABL1
- Version: 27-Jun-2013
Alternate Names:

25 Gene ID

ABL dGene Synonym

JTK7 dGene Synonym

Gene Info:

Gene Categories:

KINASE, TYROSINE KINASE

Publications:
TTD: Tyrosine-protein kinase ABL1
- Version: 2020.06.01
Alternate Names:

ABL TTD Gene Abbreviation

T63505 TTD Target ID

Gene Info:

Publications:
CGI: ABL1
- Version: 27-September-2017
Alternate Names:

Gene Info:

Publications:
MskImpact: ABL1
- Version: May-2015
Alternate Names:

Gene Info:

Gene Categories:

CLINICALLY ACTIONABLE

Publications:
FoundationOneGenes: ABL1
- Version: 03-September-2020
Alternate Names:

Gene Info:

Gene Categories:

CLINICALLY ACTIONABLE

Publications:
CarisMolecularIntelligence: ABL1
- Version: 04-September-2020
Alternate Names:

Gene Info:

Gene Categories:

CLINICALLY ACTIONABLE

Publications:
FDA: ABL1
- Version: 04-September-2020
Alternate Names:

Gene Info:

Publications:
COSMIC: ABL1
- Version: 4-Sep-2020
Alternate Names:

Gene Info:

Gene Categories:

DRUG RESISTANCE

Publications:

Mechanism of Interaction	Tyrosine-protein kinase ABL inhibitor
Direct Interaction	yes
Details of the Assay for Interaction	Two assays used: a radiometric filter-binding assay and microfluidic mobility shift technology (Caliper assay).

Trial Name	nilotinib , AMN-107,Tasigna
Novel drug target	Established target
Variant Effect	gain-of-function

Drug family	BCR-ABL inhibitor 3rd gen&Pan-TK inhibitor
Alteration	ABL1:T315I
Alteration	ABL1__BCR

Variant Effect	gain-of-function
Pathway	activation
Clinical Status	NCCN guidelines

Details of the Assay for Interaction	Inhibition of native ABL kinase activity.
Specific Action of the Ligand	Inhibition
Endogenous Drug?	False

combination therapy	[Nilotinib,Dasatinib]
Drug family	[BCR-ABL inhibitor 2nd gen]
Alteration	ABL1:T315I

Fusion protein	BCR:ABL1
Trial Name	imatinib mesylate, STI 571,Gleevec, Glivec
Novel drug target	Established target

Trial Name	XL228
Novel drug target	Established target
Mechanism of Interaction	Tyrosine-protein kinase ABL inhibitor

Trial Name	masitinib, AB1010
Novel drug target	Established target

combination therapy	Dasatinib;Venetoclax
Drug family	BCR-ABL inhibitor 2nd gen;BCL2 inhibitor
Alteration	ABL1__BCR

combination therapy	Trametinib;Imatinib
Drug family	MEK inhibitor;BCR-ABL inhibitor 1st gen&KIT inhibitor
Alteration	PRKCH:amp;ABL1__BCR

ABL1_HUMAN	Uniprot Id
P00519	Uniprot Accession
ENSG00000097007	Ensembl Gene Id

TYROSINE-PROTEIN KINASE ABL1	Uniprot Protein Name
ENSG00000097007	Ensembl Gene Id
25	Entrez Gene Id

76	HUGO Gene ID
76	HUGO Gene Symbol
ABL proto-oncogene 1, non-receptor tyrosine kinase	HUGO Gene Name

ABL1	DrugBank Gene Name
P00519	UniProt Accession
25	Entrez Gene Id

25	Entrez Gene Id
ABL1	MyCancerGenome Gene Symbol
ABL	MyCancerGenome Reported Gene Name

JTK7	GENE_SYMBOL
ABL1	GENE_SYMBOL
Tyrosine-protein kinase ABL1	UNIPROT

p150	OncoKB Gene Synonym
25	OncoKB Entrez Id
v-abl	OncoKB Gene Synonym

ABL1 Gene Record

ABL1 25 Druggable GenomeClinically ActionableDrug Resistance

Alternate Names:

Gene Info:

Gene Categories: Category Details

Publications:

Interaction Types & Directionality: allosteric modulator inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Tyrosine-protein kinase ABL inhibitor Direct Interaction yes Details of the Assay for Interaction Two assays used: a radiometric filter-binding assay and microfluidic mobility shift technology (Caliper assay).

PMIDs: None found

Sources: OncoKB GuideToPharmacology ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Trial Name nilotinib , AMN-107,Tasigna Novel drug target Established target Variant Effect gain-of-function

PMIDs: 17715389 20537386 17929114 19075254 23676790 16721371 12623848 18191450 25686603 20367437 17114651 18828913 28514312 21895409 21489624 11964322 25157968 21605905 19822896 21562040 19652056 16772610 19920925

Sources: TEND OncoKB FDA PharmGKB DoCM JAX-CKB TdgClinicalTrial CIViC DrugBank COSMIC MyCancerGenome GuideToPharmacology CGI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 10592235

Sources: DrugBank

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info:

PMIDs: 24705186

Sources: DrugBank

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Drug family BCR-ABL inhibitor 3rd gen&Pan-TK inhibitor Alteration ABL1:T315I Alteration ABL1__BCR

Sources: DTC OncoKB FDA PharmGKB DoCM TdgClinicalTrial CIViC TTD DrugBank MyCancerGenome GuideToPharmacology CGI

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Variant Effect gain-of-function Pathway activation Clinical Status NCCN guidelines

PMIDs: 14745431 15256422 23676790 11853795 20697894 12623848 19466505 20367437 17114651 18828913 15381060 21895409 21489624 11964322 24456693 18615627 25157968 14559829 21605905 21562040 21505103 19652056 12399961

Sources: OncoKB FDA PharmGKB DoCM TdgClinicalTrial TTD DrugBank COSMIC MyCancerGenome GuideToPharmacology ChemblInteractions CGI

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Tyrosine-protein kinase ABL inhibitor Direct Interaction yes Specific Action of the Ligand Inhibition

PMIDs: 18191450

Sources: CIViC MyCancerGenome GuideToPharmacology ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Details of the Assay for Interaction Inhibition of native ABL kinase activity. Specific Action of the Ligand Inhibition Endogenous Drug? False

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Tyrosine-protein kinase ABL inhibitor Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Specific Action of the Ligand Inhibition Endogenous Drug? False Direct Interaction? False

PMIDs: None found

Sources: TTD GuideToPharmacology ChemblInteractions

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 16415863

Sources: DTC

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Tyrosine-protein kinase ABL inhibitor Direct Interaction yes Specific Action of the Ligand Inhibition

PMIDs: None found

Sources: TTD GuideToPharmacology ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Tyrosine-protein kinase ABL inhibitor Direct Interaction yes Specific Action of the Ligand Inhibition

PMIDs: None found

Sources: TTD GuideToPharmacology ChemblInteractions

Interaction Types & Directionality: multitarget inhibitor (inhibitory)

Interaction Info: combination therapy [Nilotinib,Dasatinib] Drug family [BCR-ABL inhibitor 2nd gen] Alteration ABL1:T315I

PMIDs: 14745431 20537386 15256422 26758680 23676790 15705718 19779040 11853795 20697894 16775234 24367893 19466505 18191450 25686603 20367437 17701954 25207766 15381060 21895409 18818391 11964322 11752352 24456693 18615627 25157968 14559829 17016423 21562040 21505103 19652056 16772610 12399961

Sources: TEND OncoKB FDA PharmGKB DoCM JAX-CKB TdgClinicalTrial CIViC DrugBank COSMIC MyCancerGenome GuideToPharmacology ChemblInteractions CGI

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Fusion protein BCR:ABL1 Trial Name imatinib mesylate, STI 571,Gleevec, Glivec Novel drug target Established target

PMIDs: 20537386 26758680 16205964 19075254 27125982 15930265 15917650 16775234 24367893 12623848 16630177 18191450 25686603 25207766 22148584 22371878 15799618 15949566 16153117 12476305 15194504 24681986

Sources: NCI TEND DTC OncoKB FDA PharmGKB JAX-CKB TdgClinicalTrial CIViC DrugBank COSMIC MyCancerGenome GuideToPharmacology CGI

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Tyrosine-protein kinase ABL inhibitor Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Tyrosine-protein kinase ABL inhibitor Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Tyrosine-protein kinase ABL inhibitor Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 8683981

Interaction Types & Directionality:

allosteric modulator

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Tyrosine-protein kinase ABL inhibitor

Direct Interaction yes

Details of the Assay for Interaction Two assays used: a radiometric filter-binding assay and microfluidic mobility shift technology (Caliper assay).

PMIDs:
None found

Sources:
OncoKB GuideToPharmacology ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name nilotinib , AMN-107,Tasigna

Novel drug target Established target

Variant Effect gain-of-function

PMIDs:
17715389 20537386 17929114 19075254 23676790 16721371 12623848 18191450 25686603 20367437 17114651 18828913 28514312 21895409 21489624 11964322 25157968 21605905 19822896 21562040 19652056 16772610 19920925

Sources:
TEND OncoKB FDA PharmGKB DoCM JAX-CKB TdgClinicalTrial CIViC DrugBank COSMIC MyCancerGenome GuideToPharmacology CGI

Interaction Types & Directionality:

n/a

PMIDs:
10592235

Sources:
DrugBank

Interaction Types & Directionality:

antagonist (inhibitory)

PMIDs:
24705186

Sources:
DrugBank

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Drug family BCR-ABL inhibitor 3rd gen&Pan-TK inhibitor

Alteration ABL1:T315I

Alteration ABL1__BCR

Sources:
DTC OncoKB FDA PharmGKB DoCM TdgClinicalTrial CIViC TTD DrugBank MyCancerGenome GuideToPharmacology CGI

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Variant Effect gain-of-function

Pathway activation

Clinical Status NCCN guidelines

PMIDs:
14745431 15256422 23676790 11853795 20697894 12623848 19466505 20367437 17114651 18828913 15381060 21895409 21489624 11964322 24456693 18615627 25157968 14559829 21605905 21562040 21505103 19652056 12399961

Sources:
OncoKB FDA PharmGKB DoCM TdgClinicalTrial TTD DrugBank COSMIC MyCancerGenome GuideToPharmacology ChemblInteractions CGI

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Tyrosine-protein kinase ABL inhibitor

Direct Interaction yes

Specific Action of the Ligand Inhibition

PMIDs:
18191450

Sources:
CIViC MyCancerGenome GuideToPharmacology ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction Inhibition of native ABL kinase activity.

Specific Action of the Ligand Inhibition

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Tyrosine-protein kinase ABL inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
TTD GuideToPharmacology ChemblInteractions

Interaction Types & Directionality:

n/a

PMIDs:
16415863

Sources:
DTC

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Tyrosine-protein kinase ABL inhibitor

Direct Interaction yes

Specific Action of the Ligand Inhibition

PMIDs:
None found

Sources:
TTD GuideToPharmacology ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Tyrosine-protein kinase ABL inhibitor

Direct Interaction yes

Specific Action of the Ligand Inhibition

PMIDs:
None found

Sources:
TTD GuideToPharmacology ChemblInteractions

Interaction Types & Directionality:

multitarget

inhibitor (inhibitory)

Interaction Info:

combination therapy [Nilotinib,Dasatinib]

Drug family [BCR-ABL inhibitor 2nd gen]

Alteration ABL1:T315I

PMIDs:
14745431 20537386 15256422 26758680 23676790 15705718 19779040 11853795 20697894 16775234 24367893 19466505 18191450 25686603 20367437 17701954 25207766 15381060 21895409 18818391 11964322 11752352 24456693 18615627 25157968 14559829 17016423 21562040 21505103 19652056 16772610 12399961

Sources:
TEND OncoKB FDA PharmGKB DoCM JAX-CKB TdgClinicalTrial CIViC DrugBank COSMIC MyCancerGenome GuideToPharmacology ChemblInteractions CGI

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Fusion protein BCR:ABL1

Trial Name imatinib mesylate, STI 571,Gleevec, Glivec

Novel drug target Established target

PMIDs:
20537386 26758680 16205964 19075254 27125982 15930265 15917650 16775234 24367893 12623848 16630177 18191450 25686603 25207766 22148584 22371878 15799618 15949566 16153117 12476305 15194504 24681986

Sources:
NCI TEND DTC OncoKB FDA PharmGKB JAX-CKB TdgClinicalTrial CIViC DrugBank COSMIC MyCancerGenome GuideToPharmacology CGI

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Tyrosine-protein kinase ABL inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Tyrosine-protein kinase ABL inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Tyrosine-protein kinase ABL inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

n/a

PMIDs:
8683981

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
23239810 28597393

Sources:
DrugBank

Interaction Types & Directionality:

n/a

Interaction Info:

Alteration ABL1:T315I

Drug family VEGFR inhibitor

PMIDs:
25686603