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CHEBI ONTOLOGY - ANNOTATIONS

The Chemical Entities of Biological Interest (ChEBI) ontology is downloaded weekly from EMBL-EBI at http://www.ebi.ac.uk/chebi/. The data is made available under the Creative Commons License (CC BY 3.0, http://creativecommons.org/licenses/by/3.0/). For more information see: Degtyarenko et al. (2008) ChEBI: a database and ontology for chemical entities of biological interest. Nucleic Acids Res. 36, D344–D350.

Term:dactolisib
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Accession:CHEBI:71952 term browser browse the term
Definition:An imidazoquinoline that is 3-methyl-2-oxo-2,3-dihydro-1H-imidazo[4,5-c]quinoline substituted at position 1 by a 4-(1-cyanoisopropyl)phenyl group and at position 8 by a quinolin-3-yl group. A dual PI3K/mTOR inhibitor used in cancer treatment.
Synonyms:exact_synonym: 2-methyl-2-{4-[3-methyl-2-oxo-8-(quinolin-3-yl)-2,3-dihydro-1H-imidazo[4,5-c]quinolin-1-yl]phenyl}propanenitrile
 related_synonym: BEZ-235;   BEZ235;   Formula=C30H23N5O;   InChI=1S/C30H23N5O/c1-30(2,18-31)22-9-11-23(12-10-22)35-28-24-15-19(21-14-20-6-4-5-7-25(20)32-16-21)8-13-26(24)33-17-27(28)34(3)29(35)36/h4-17H,1-3H3;   InChIKey=JOGKUKXHTYWRGZ-UHFFFAOYSA-N;   NVP-BEZ 235;   NVP-BEZ235;   NVPBEZ235;   SMILES=Cn1c2cnc3ccc(cc3c2n(-c2ccc(cc2)C(C)(C)C#N)c1=O)-c1cnc2ccccc2c1
 alt_id: MESH:C531198
 xref: CAS:915019-65-7;   LINCS:LSM-4255
 xref_mesh: MESH:C531198
 xref: PMID:22020918;   PMID:22154651;   PMID:22218692;   PMID:22287733;   PMID:22299028;   PMID:22355272;   PMID:22401294;   PMID:22415236;   PMID:22452803;   PMID:22560334;   PMID:22662154;   PMID:22727754;   PMID:22858987;   PMID:22895065;   PMID:22920938;   PMID:22960230;   PMID:22989521;   PMID:23077520;   PMID:23215722;   PMID:23232026;   PMID:23300274;   PMID:23319394;   PMID:23319457;   PMID:23321494;   PMID:23343422;   Patent:WO2006122806;   Patent:WO2008064093;   Reaxys:12748665


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dactolisib term browser
Symbol Object Name Qualifiers Evidence Notes Source PubMed Reference(s) RGD Reference(s) Position
G Akt1 AKT serine/threonine kinase 1 decreases expression
decreases phosphorylation
multiple interactions
ISO dactolisib results in decreased expression of AKT1 protein modified form
dactolisib results in decreased phosphorylation of AKT1 protein
dactolisib inhibits the reaction [EGF protein results in increased phosphorylation of AKT1 protein]; PD 0325901 promotes the reaction [dactolisib results in decreased phosphorylation of AKT1 protein]
dactolisib inhibits the reaction [INS1 protein results in increased phosphorylation of AKT1 protein]; LEPR affects the reaction [dactolisib results in decreased phosphorylation of AKT1 protein]
CTD PMID:19435893 PMID:21464613 PMID:22415236 PMID:22949526 PMID:23151917 PMID:24758408 PMID:25640480 NCBI chr 6:131,713,716...131,735,319 JBrowse link
G Bax BCL2 associated X, apoptosis regulator multiple interactions ISO Chloroquine promotes the reaction [dactolisib affects the folding of and results in increased activity of BAX protein]; dactolisib affects the folding of and results in increased activity of BAX protein; dactolisib promotes the reaction [Chloroquine affects the folding of and results in increased activity of BAX protein] CTD PMID:23151917 NCBI chr 1:95,940,001...95,945,407 JBrowse link
G Bcl2l1 Bcl2-like 1 affects expression ISO dactolisib affects the expression of BCL2L1 protein CTD PMID:25640480 NCBI chr 3:141,253,508...141,304,582 JBrowse link
G Bcl2l11 BCL2 like 11 affects expression ISO dactolisib affects the expression of BCL2L11 protein CTD PMID:25640480 NCBI chr 3:115,366,783...115,404,068 JBrowse link
G Birc5 baculoviral IAP repeat-containing 5 decreases expression ISO dactolisib results in decreased expression of BIRC5 protein CTD PMID:22729845 NCBI chr10:103,072,530...103,081,382 JBrowse link
G Casp3 caspase 3 increases activity
multiple interactions
increases cleavage
ISO dactolisib results in increased activity of CASP3 protein
Chloroquine promotes the reaction [dactolisib results in increased cleavage of CASP3 protein]; dactolisib promotes the reaction [Chloroquine results in increased cleavage of CASP3 protein]
CTD PMID:21372221 PMID:23151917 NCBI chr16:45,662,910...45,681,171 JBrowse link
G Casp9 caspase 9 multiple interactions
increases cleavage
ISO Chloroquine promotes the reaction [dactolisib results in increased cleavage of CASP9 protein]; dactolisib promotes the reaction [Chloroquine results in increased cleavage of CASP9 protein] CTD PMID:23151917 NCBI chr 5:154,108,872...154,126,628 JBrowse link
G Ccnd1 cyclin D1 decreases phosphorylation ISO dactolisib results in decreased phosphorylation of CCND1 protein CTD PMID:23651616 NCBI chr 1:200,089,002...200,098,524 JBrowse link
G Cdkn1a cyclin-dependent kinase inhibitor 1A increases expression ISO dactolisib results in increased expression of CDKN1A protein CTD PMID:23651616 NCBI chr20:7,149,177...7,159,727 JBrowse link
G Ctsb cathepsin B affects localization
multiple interactions
ISO dactolisib affects the localization of CTSB protein
[Chloroquine co-treated with dactolisib] affects the localization of CTSB protein
CTD PMID:23151917 NCBI chr15:37,389,636...37,410,508 JBrowse link
G Egf epidermal growth factor multiple interactions ISO dactolisib inhibits the reaction [EGF protein results in increased phosphorylation of AKT1 protein] CTD PMID:24758408 NCBI chr 2:218,219,408...218,302,370 JBrowse link
G Eif4ebp1 eukaryotic translation initiation factor 4E binding protein 1 decreases phosphorylation
multiple interactions
increases response to substance
ISO dactolisib results in decreased phosphorylation of EIF4EBP1 protein
Ku 0063794 inhibits the reaction [dactolisib results in decreased phosphorylation of EIF4EBP1 protein]; PD 0325901 promotes the reaction [dactolisib results in decreased phosphorylation of EIF4EBP1 protein]
EIF4EBP1 protein modified form results in increased susceptibility to dactolisib
CTD PMID:21372221 PMID:22415236 PMID:23151917 PMID:25640480 NCBI chr16:64,792,595...64,805,984 JBrowse link
G Lepr leptin receptor multiple interactions ISO LEPR affects the reaction [dactolisib results in decreased phosphorylation of AKT1 protein] CTD PMID:22949526 NCBI chr 5:116,294,409...116,477,904 JBrowse link
G Map1lc3a microtubule-associated protein 1 light chain 3 alpha increases metabolic processing
affects localization
ISO dactolisib results in increased metabolism of MAP1LC3A protein
dactolisib affects the localization of MAP1LC3A protein
CTD PMID:23651616 NCBI chr 3:143,783,024...143,784,670 JBrowse link
G Mapk1 mitogen activated protein kinase 1 multiple interactions ISO dactolisib promotes the reaction [PD 0325901 results in decreased phosphorylation of MAPK1 protein] CTD PMID:22415236 NCBI chr11:83,957,813...84,023,629 JBrowse link
G Mapk3 mitogen activated protein kinase 3 multiple interactions ISO dactolisib promotes the reaction [PD 0325901 results in decreased phosphorylation of MAPK3 protein] CTD PMID:22415236 NCBI chr 1:181,366,646...181,372,863 JBrowse link
G Mcl1 MCL1 apoptosis regulator, BCL2 family member affects expression
multiple interactions
ISO dactolisib affects the expression of MCL1 protein
[dactolisib co-treated with (+)-JQ1 compound] affects the expression of MCL1 protein
CTD PMID:25640480 NCBI chr 2:183,219,137...183,235,676 JBrowse link
G Ogt O-linked N-acetylglucosamine (GlcNAc) transferase increases response to substance ISO OGT mutant form results in increased susceptibility to dactolisib CTD PMID:23029544 NCBI chr  X:66,771,278...66,816,148 JBrowse link
G Oxsr1 oxidative stress responsive kinase 1 multiple interactions
decreases phosphorylation
ISO dactolisib inhibits the reaction [INS1 protein results in increased phosphorylation of OXSR1 protein]
dactolisib results in decreased phosphorylation of OXSR1 protein
CTD PMID:22949526 NCBI chr 8:118,972,754...119,062,102 JBrowse link
G Parp1 poly (ADP-ribose) polymerase 1 increases cleavage ISO dactolisib results in increased cleavage of PARP1 protein CTD PMID:21464613 NCBI chr13:92,307,593...92,339,406 JBrowse link
G Pik3ca phosphatidylinositol-4,5-bisphosphate 3-kinase, catalytic subunit alpha increases response to substance
decreases response to substance
ISO PIK3CA results in increased susceptibility to dactolisib
PIK3CA results in decreased susceptibility to dactolisib
CTD PMID:21372221 PMID:21633166 NCBI chr 2:115,175,275...115,249,034 JBrowse link
G Pten phosphatase and tensin homolog increases response to substance ISO PTEN gene mutant form results in increased susceptibility to dactolisib CTD PMID:21372221 NCBI chr 1:230,631,303...230,696,754 JBrowse link
G Rb1 RB transcriptional corepressor 1 decreases expression ISO dactolisib results in decreased expression of RB1 protein modified form CTD PMID:23651616 NCBI chr15:48,371,295...48,502,473 JBrowse link
G Rps6 ribosomal protein S6 multiple interactions
decreases phosphorylation
ISO PD 0325901 promotes the reaction [dactolisib results in decreased phosphorylation of RPS6 protein] CTD PMID:21372221 PMID:21464613 PMID:21498705 PMID:22415236 PMID:23151917 PMID:25640480 NCBI chr 5:101,371,716...101,374,576 JBrowse link
G Rps6kb1 ribosomal protein S6 kinase B1 decreases phosphorylation ISO dactolisib results in decreased phosphorylation of RPS6KB1 protein CTD PMID:21464613 NCBI chr10:71,323,777...71,367,908 JBrowse link
G Slc12a3 solute carrier family 12 member 3 multiple interactions
decreases phosphorylation
ISO dactolisib inhibits the reaction [INS1 protein results in increased phosphorylation of SLC12A3 protein]
dactolisib results in decreased phosphorylation of SLC12A3 protein
CTD PMID:22949526 NCBI chr19:10,630,649...10,679,250 JBrowse link
G Sqstm1 sequestosome 1 multiple interactions
decreases expression
ISO bafilomycin A1 inhibits the reaction [dactolisib results in decreased expression of SQSTM1 protein]; Chloroquine inhibits the reaction [dactolisib results in decreased expression of SQSTM1 protein] CTD PMID:23151917 PMID:23651616 NCBI chr10:34,525,517...34,536,685 JBrowse link
G Stk39 serine threonine kinase 39 multiple interactions
decreases phosphorylation
ISO dactolisib inhibits the reaction [INS1 protein results in increased phosphorylation of STK39 protein]
dactolisib results in decreased phosphorylation of STK39 protein
CTD PMID:22949526 NCBI chr 3:52,913,583...53,179,060 JBrowse link

Term paths to the root
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  CHEBI ontology 19762
    chemical entity 19762
      group 19681
        pseudohalo group 3223
          cyano group 3223
            nitrile 3223
              dactolisib 28
Path 2
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  CHEBI ontology 19762
    subatomic particle 19760
      composite particle 19760
        hadron 19760
          baryon 19760
            nucleon 19760
              atomic nucleus 19760
                atom 19760
                  main group element atom 19651
                    p-block element atom 19651
                      carbon group element atom 19570
                        carbon atom 19560
                          organic molecular entity 19560
                            organic group 18611
                              organic divalent group 18602
                                organodiyl group 18602
                                  carbonyl group 18519
                                    carbonyl compound 18519
                                      carboxylic acid 18195
                                        carboacyl group 17423
                                          univalent carboacyl group 17423
                                            carbamoyl group 17230
                                              carboxamide 17230
                                                monocarboxylic acid amide 14854
                                                  urea 5099
                                                    ureas 5097
                                                      dactolisib 28
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