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ABL1 Gene Record

  • Summary
  • Interactions
  • Claims
  • 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:

Disclaimer: This resource is intended for purely research purposes. It should not be used for emergencies or medical or professional advice.

A finding of a drug-gene interaction or potentially druggable category does not necessarily indicate effectiveness (or lack thereof) of any drug or treatment regimen. A finding of no interaction or no potentially druggable category does not necessarily indicate lack of effectiveness of any drug or treatment regimen. Drug-gene interactions or potentially druggable categories are not presented in ranked order of potential or predicted efficacy.

The dgidb.org website does not provide any medical or healthcare products, services or advice, and is not for medical emergencies or urgent situations. IF YOU THINK YOU MAY HAVE A MEDICAL EMERGENCY, CALL YOUR DOCTOR OR 911 IMMEDIATELY. Information contained on this website is not a substitute for a doctor's medical judgment or advice. We recommend that you discuss your specific, individual health concerns with your doctor or health care professional.

DGIdb (v4.2.0 - sha1 afd9f30b) • Last updated 2020-10-21