Compounds > 3-(6-isobutyl-9-methoxy-1,4-dioxo-1,2,3,4,6,7,12,12a-octahydropyrazino(1',2'-1,6)pyrido(3,4-b)indol-3-yl)propionic acid tert-butyl ester
Page last updated: 2024-08-03 21:38:55
3-(6-isobutyl-9-methoxy-1,4-dioxo-1,2,3,4,6,7,12,12a-octahydropyrazino(1',2'-1,6)pyrido(3,4-b)indol-3-yl)propionic acid tert-butyl ester
Description
3-(6-isobutyl-9-methoxy-1,4-dioxo-1,2,3,4,6,7,12,12a-octahydropyrazino(1',2'-1,6)pyrido(3,4-b)indol-3-yl)propionic acid tert-butyl ester: a breast cancer resistance protein (BCRP) inhibitor; structure in first source [MeSH]
Cross-References
| ID Source | ID |
|---|
| PubMed CID | 69534441 |
| SCHEMBL ID | 5696166 |
| MeSH ID | M0536777 |
Synonyms (4)
| Synonym |
|---|
| 3-(6-isobutyl-9-methoxy-1,4-dioxo-1,2,3,4,6,7,12,12a-octahydropyrazino(1',2'-1,6)pyrido(3,4-b)indol-3-yl)propionic acid tert-butyl ester |
| FT-0670686 |
| SCHEMBL5696166 |
| HMS3740M21 |
Research
Studies (67)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 3 (4.48) | 29.6817 |
| 2010's | 55 (82.09) | 24.3611 |
| 2020's | 9 (13.43) | 2.80 |
Study Types
| Publication Type | This drug (%) | All Drugs (%) |
|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 1 (1.45%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 68 (98.55%) | 84.16% |
| Substance | Studies | Classes | Roles | First Year | Last Year | Average Age | Relationship Strength | Trials | pre-1990 | 1990's | 2000's | 2010's | post-2020 |
|---|
| aminolevulinic acid | | 4-oxo monocarboxylic acid;
amino acid zwitterion;
delta-amino acid | antineoplastic agent;
dermatologic drug;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
photosensitizing agent;
plant metabolite;
prodrug;
Saccharomyces cerevisiae metabolite | 2012 | 2019 | 8.2 | low | 0 | 0 | 0 | 0 | 4 | 0 |
| acetic acid | | monocarboxylic acid | antimicrobial food preservative;
Daphnia magna metabolite;
food acidity regulator;
protic solvent | 2016 | 2016 | 8.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| benzoic acid | | benzoic acids | algal metabolite;
antimicrobial food preservative;
drug allergen;
EC 1.13.11.33 (arachidonate 15-lipoxygenase) inhibitor;
EC 3.1.1.3 (triacylglycerol lipase) inhibitor;
human xenobiotic metabolite;
plant metabolite | 2016 | 2016 | 8.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| glycine | | alpha-amino acid;
amino acid zwitterion;
proteinogenic amino acid;
serine family amino acid | EC 2.1.2.1 (glycine hydroxymethyltransferase) inhibitor;
fundamental metabolite;
hepatoprotective agent;
micronutrient;
neurotransmitter;
NMDA receptor agonist;
nutraceutical | 2013 | 2013 | 11.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| niacinamide | | pyridine alkaloid;
pyridinecarboxamide;
vitamin B3 | anti-inflammatory agent;
antioxidant;
cofactor;
EC 2.4.2.30 (NAD(+) ADP-ribosyltransferase) inhibitor;
EC 3.5.1.98 (histone deacetylase) inhibitor;
Escherichia coli metabolite;
geroprotector;
human urinary metabolite;
metabolite;
mouse metabolite;
neuroprotective agent;
Saccharomyces cerevisiae metabolite;
Sir2 inhibitor | 2018 | 2018 | 6.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| uric acid | | uric acid | Escherichia coli metabolite;
human metabolite;
mouse metabolite | 2012 | 2012 | 12.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| 2-amino-1-methyl-6-phenylimidazo(4,5-b)pyridine | | imidazopyridine;
primary amino compound | carcinogenic agent;
mutagen | 2015 | 2015 | 9.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| aristolochic acid i | | aristolochic acids;
aromatic ether;
C-nitro compound;
cyclic acetal;
monocarboxylic acid;
organic heterotetracyclic compound | carcinogenic agent;
metabolite;
mutagen;
nephrotoxin;
toxin | 2016 | 2016 | 8.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| verapamil | | aromatic ether;
nitrile;
polyether;
tertiary amino compound | | 2011 | 2020 | 8.8 | low | 0 | 0 | 0 | 0 | 6 | 0 |
| dipyridamole | | piperidines;
pyrimidopyrimidine;
tertiary amino compound;
tetrol | adenosine phosphodiesterase inhibitor;
EC 3.5.4.4 (adenosine deaminase) inhibitor;
platelet aggregation inhibitor;
vasodilator agent | 2018 | 2018 | 6.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| fexofenadine | | piperidines;
tertiary amine | anti-allergic agent;
H1-receptor antagonist | 2013 | 2013 | 11.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| hydroxyurea | | one-carbon compound;
ureas | antimetabolite;
antimitotic;
antineoplastic agent;
DNA synthesis inhibitor;
EC 1.17.4.1 (ribonucleoside-diphosphate reductase) inhibitor;
genotoxin;
immunomodulator;
radical scavenger;
teratogenic agent | 2021 | 2021 | 3.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| indomethacin | | aromatic ether;
indole-3-acetic acids;
monochlorobenzenes;
N-acylindole | analgesic;
drug metabolite;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
environmental contaminant;
gout suppressant;
non-steroidal anti-inflammatory drug;
xenobiotic metabolite;
xenobiotic | 2016 | 2016 | 8.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| ketoconazole | | dichlorobenzene;
dioxolane;
ether;
imidazoles;
N-acylpiperazine;
N-arylpiperazine | | 2013 | 2013 | 11.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| lamotrigine | | 1,2,4-triazines;
dichlorobenzene;
primary arylamine | anticonvulsant;
antidepressant;
antimanic drug;
calcium channel blocker;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
environmental contaminant;
excitatory amino acid antagonist;
geroprotector;
non-narcotic analgesic;
xenobiotic | 2015 | 2015 | 9.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| 2-(4-morpholinyl)-8-phenyl-4h-1-benzopyran-4-one | | chromones;
morpholines;
organochlorine compound | autophagy inhibitor;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor;
geroprotector | 2014 | 2014 | 10.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| mitoxantrone | | dihydroxyanthraquinone | analgesic;
antineoplastic agent | 2012 | 2016 | 9.7 | low | 0 | 0 | 0 | 0 | 6 | 0 |
| prazosin | | aromatic ether;
furans;
monocarboxylic acid amide;
piperazines;
quinazolines | alpha-adrenergic antagonist;
antihypertensive agent;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor | 2011 | 2020 | 7.3 | low | 0 | 0 | 0 | 0 | 3 | 0 |
| protoporphyrin ix | | | | 2012 | 2019 | 8.2 | low | 0 | 0 | 0 | 0 | 4 | 0 |
| rolipram | | pyrrolidin-2-ones | antidepressant;
EC 3.1.4.* (phosphoric diester hydrolase) inhibitor | 2013 | 2013 | 11.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| sulfasalazine | | | | 2013 | 2013 | 11.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| gatifloxacin | | N-arylpiperazine;
organofluorine compound;
quinolinemonocarboxylic acid;
quinolone antibiotic;
quinolone | antiinfective agent;
antimicrobial agent;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor | 2010 | 2010 | 14.0 | low | 0 | 0 | 0 | 1 | 0 | 0 |
| temozolomide | | imidazotetrazine;
monocarboxylic acid amide;
triazene derivative | alkylating agent;
antineoplastic agent;
prodrug | 2017 | 2022 | 4.5 | low | 0 | 0 | 0 | 0 | 1 | 1 |
| terfenadine | | diarylmethane | | 2013 | 2013 | 11.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| tolmetin | | aromatic ketone;
monocarboxylic acid;
pyrroles | EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
non-steroidal anti-inflammatory drug | 2013 | 2013 | 11.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| estrone | | 17-oxo steroid;
3-hydroxy steroid;
phenolic steroid;
phenols | antineoplastic agent;
bone density conservation agent;
estrogen;
human metabolite;
mouse metabolite | 2016 | 2016 | 8.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| bisphenol a | | bisphenol | endocrine disruptor;
environmental contaminant;
xenobiotic;
xenoestrogen | 2021 | 2021 | 3.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| bis(4-hydroxyphenyl)sulfone | | bisphenol;
sulfone | endocrine disruptor;
metabolite | 2021 | 2021 | 3.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| taurocholic acid | | amino sulfonic acid;
bile acid taurine conjugate | human metabolite | 2021 | 2021 | 3.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| rotenone | | organic heteropentacyclic compound;
rotenones | antineoplastic agent;
metabolite;
mitochondrial NADH:ubiquinone reductase inhibitor;
phytogenic insecticide;
piscicide;
toxin | 2012 | 2012 | 12.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| 4-butyrolactone | | butan-4-olide | metabolite;
neurotoxin | 2014 | 2014 | 10.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| pyrroles | | pyrrole;
secondary amine | | 2013 | 2013 | 11.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| quinazolines | | azaarene;
mancude organic heterobicyclic parent;
ortho-fused heteroarene;
quinazolines | | 2008 | 2014 | 12.3 | low | 0 | 0 | 0 | 1 | 2 | 0 |
| acridines | | acridines;
mancude organic heterotricyclic parent;
polycyclic heteroarene | genotoxin | 2009 | 2017 | 12.0 | low | 0 | 0 | 0 | 3 | 2 | 0 |
| benzoxazoles | | 1,3-benzoxazoles;
mancude organic heterobicyclic parent | | 2015 | 2015 | 9.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| 4,4'-bisphenol f | | bisphenol;
diarylmethane | environmental food contaminant;
xenoestrogen | 2021 | 2021 | 3.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| erythromycin | | cyclic ketone;
erythromycin | | 2010 | 2010 | 14.0 | low | 0 | 0 | 0 | 1 | 0 | 0 |
| amiloride | | aromatic amine;
guanidines;
organochlorine compound;
pyrazines | diuretic;
sodium channel blocker | 2021 | 2021 | 3.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| camptothecin | | delta-lactone;
pyranoindolizinoquinoline;
quinoline alkaloid;
tertiary alcohol | antineoplastic agent;
EC 5.99.1.2 (DNA topoisomerase) inhibitor;
genotoxin;
plant metabolite | 2012 | 2012 | 12.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| ursodeoxycholic acid | | bile acid;
C24-steroid;
dihydroxy-5beta-cholanic acid | human metabolite;
mouse metabolite | 2018 | 2018 | 6.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| 2-amino-3-methylimidazo(4,5-f)quinoline | | imidazoquinoline | carcinogenic agent | 2010 | 2010 | 14.0 | low | 0 | 0 | 0 | 1 | 0 | 0 |
| pravastatin | | 3-hydroxy carboxylic acid;
carbobicyclic compound;
carboxylic ester;
hydroxy monocarboxylic acid;
secondary alcohol;
statin (semi-synthetic) | anticholesteremic drug;
environmental contaminant;
metabolite;
xenobiotic | 2016 | 2016 | 8.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| raloxifene hydrochloride | | hydrochloride | bone density conservation agent;
estrogen antagonist;
estrogen receptor modulator | 2015 | 2015 | 9.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| topotecan | | pyranoindolizinoquinoline | antineoplastic agent;
EC 5.99.1.2 (DNA topoisomerase) inhibitor | 2012 | 2013 | 11.7 | low | 0 | 0 | 0 | 0 | 3 | 0 |
| irinotecan | | carbamate ester;
delta-lactone;
N-acylpiperidine;
pyranoindolizinoquinoline;
ring assembly;
tertiary alcohol;
tertiary amino compound | antineoplastic agent;
apoptosis inducer;
EC 5.99.1.2 (DNA topoisomerase) inhibitor;
prodrug | 2012 | 2012 | 12.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| adenosine | | adenosines;
purines D-ribonucleoside | analgesic;
anti-arrhythmia drug;
fundamental metabolite;
human metabolite;
vasodilator agent | 2008 | 2016 | 11.3 | medium | 0 | 0 | 0 | 6 | 32 | 0 |
| nelfinavir | | aryl sulfide;
benzamides;
organic heterobicyclic compound;
phenols;
secondary alcohol;
tertiary amino compound | antineoplastic agent;
HIV protease inhibitor | 2009 | 2009 | 15.0 | low | 0 | 0 | 0 | 1 | 0 | 0 |
| st 679 | | N-acyl-amino acid | | 2013 | 2013 | 11.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| toxoflavin | | carbonyl compound;
pyrimidotriazine | antibacterial agent;
antineoplastic agent;
apoptosis inducer;
bacterial metabolite;
toxin;
virulence factor;
Wnt signalling inhibitor | 2008 | 2008 | 16.0 | low | 0 | 0 | 0 | 1 | 0 | 0 |
| triazoles | | 1,2,3-triazole | | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| firefly luciferin | | 1,3-thiazolemonocarboxylic acid;
benzothiazoles;
imidothioate | luciferin | 2013 | 2013 | 11.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| aminomalonic acid | | amino dicarboxylic acid | Daphnia magna metabolite;
human metabolite | 2015 | 2015 | 9.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| tryptoquivaline | | | | 2010 | 2018 | 10.0 | low | 0 | 0 | 0 | 1 | 1 | 0 |
| benzamil | | guanidines;
pyrazines | | 2021 | 2021 | 3.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| 2,3-bis(3'-hydroxybenzyl)butyrolactone | | lignan | | 2014 | 2014 | 10.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| elacridar | | | | 2009 | 2017 | 12.0 | low | 0 | 0 | 0 | 3 | 2 | 0 |
| imatinib mesylate | | methanesulfonate salt | anticoronaviral agent;
antineoplastic agent;
apoptosis inducer;
tyrosine kinase inhibitor | 2010 | 2013 | 12.5 | low | 0 | 0 | 0 | 1 | 1 | 0 |
| gefitinib | | aromatic ether;
monochlorobenzenes;
monofluorobenzenes;
morpholines;
quinazolines;
secondary amino compound;
tertiary amino compound | antineoplastic agent;
epidermal growth factor receptor antagonist | 2013 | 2013 | 11.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| methotrexate | | dicarboxylic acid;
monocarboxylic acid amide;
pteridines | abortifacient;
antimetabolite;
antineoplastic agent;
antirheumatic drug;
dermatologic drug;
DNA synthesis inhibitor;
EC 1.5.1.3 (dihydrofolate reductase) inhibitor;
immunosuppressive agent | 2012 | 2012 | 12.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| tolmetin glycinamide | | | | 2013 | 2013 | 11.0 | high | 0 | 0 | 0 | 0 | 1 | 0 |
| tariquidar | | benzamides | | 2010 | 2018 | 10.7 | low | 0 | 0 | 0 | 1 | 2 | 0 |
| bazedoxifene | | phenylindole | | 2016 | 2016 | 8.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| naproxen | | methoxynaphthalene;
monocarboxylic acid | antipyretic;
cyclooxygenase 1 inhibitor;
cyclooxygenase 2 inhibitor;
drug allergen;
environmental contaminant;
gout suppressant;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
xenobiotic | 2013 | 2013 | 11.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| erlotinib hydrochloride | | hydrochloride;
terminal acetylenic compound | antineoplastic agent;
protein kinase inhibitor | 2014 | 2014 | 10.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| lapatinib | | furans;
organochlorine compound;
organofluorine compound;
quinazolines | antineoplastic agent;
tyrosine kinase inhibitor | 2008 | 2008 | 16.0 | low | 0 | 0 | 0 | 1 | 0 | 0 |
| sorafenib | | (trifluoromethyl)benzenes;
aromatic ether;
monochlorobenzenes;
phenylureas;
pyridinecarboxamide | angiogenesis inhibitor;
anticoronaviral agent;
antineoplastic agent;
EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor;
ferroptosis inducer;
tyrosine kinase inhibitor | 2018 | 2018 | 6.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| pheophorbide a | | | | 2010 | 2010 | 14.0 | low | 0 | 0 | 0 | 1 | 0 | 0 |
| quinidine | | cinchona alkaloid | alpha-adrenergic antagonist;
anti-arrhythmia drug;
antimalarial;
drug allergen;
EC 1.14.13.181 (13-deoxydaunorubicin hydroxylase) inhibitor;
EC 3.6.3.44 (xenobiotic-transporting ATPase) inhibitor;
muscarinic antagonist;
P450 inhibitor;
potassium channel blocker;
sodium channel blocker | 2010 | 2020 | 8.7 | low | 0 | 0 | 0 | 1 | 2 | 0 |
| lignans | | | | 2014 | 2014 | 10.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| posaconazole | | aromatic ether;
conazole antifungal drug;
N-arylpiperazine;
organofluorine compound;
oxolanes;
triazole antifungal drug;
triazoles | trypanocidal drug | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| glycosides | | | | 2012 | 2012 | 12.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| s 1033 | | (trifluoromethyl)benzenes;
imidazoles;
pyridines;
pyrimidines;
secondary amino compound;
secondary carboxamide | anticoronaviral agent;
antineoplastic agent;
tyrosine kinase inhibitor | 2013 | 2013 | 11.0 | low | 0 | 0 | 0 | 0 | 2 | 0 |
| digoxin | | cardenolide glycoside;
steroid saponin | anti-arrhythmia drug;
cardiotonic drug;
EC 3.6.3.9 (Na(+)/K(+)-transporting ATPase) inhibitor;
epitope | 2013 | 2013 | 11.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| estrone sulfate | | 17-oxo steroid;
steroid sulfate | human metabolite;
mouse metabolite | 2016 | 2016 | 8.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| ly335979 | | carbopolycyclic compound | | 2011 | 2020 | 8.2 | low | 0 | 0 | 0 | 0 | 5 | 0 |
| ovalbumin | | | | 2013 | 2013 | 11.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| rhodamine 123 | | organic cation;
xanthene dye | fluorochrome | 2012 | 2012 | 12.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| quercetin | | 7-hydroxyflavonol;
pentahydroxyflavone | antibacterial agent;
antineoplastic agent;
antioxidant;
Aurora kinase inhibitor;
chelator;
EC 1.10.99.2 [ribosyldihydronicotinamide dehydrogenase (quinone)] inhibitor;
geroprotector;
phytoestrogen;
plant metabolite;
protein kinase inhibitor;
radical scavenger | 2016 | 2016 | 8.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| apigenin | | trihydroxyflavone | antineoplastic agent;
metabolite | 2015 | 2015 | 9.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| luteolin | | 3'-hydroxyflavonoid;
tetrahydroxyflavone | angiogenesis inhibitor;
anti-inflammatory agent;
antineoplastic agent;
apoptosis inducer;
c-Jun N-terminal kinase inhibitor;
EC 2.3.1.85 (fatty acid synthase) inhibitor;
immunomodulator;
nephroprotective agent;
plant metabolite;
radical scavenger;
vascular endothelial growth factor receptor antagonist | 2014 | 2014 | 10.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| genistein | | 7-hydroxyisoflavones | antineoplastic agent;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor;
geroprotector;
human urinary metabolite;
phytoestrogen;
plant metabolite;
tyrosine kinase inhibitor | 2012 | 2012 | 12.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| amphotericin b | | antibiotic antifungal drug;
macrolide antibiotic;
polyene antibiotic | antiamoebic agent;
antiprotozoal drug;
bacterial metabolite | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| chrysin | | 7-hydroxyflavonol;
dihydroxyflavone | anti-inflammatory agent;
antineoplastic agent;
antioxidant;
EC 2.7.11.18 (myosin-light-chain kinase) inhibitor;
hepatoprotective agent;
plant metabolite | 2015 | 2015 | 9.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| forsythiaside | | hydroxycinnamic acid | | 2012 | 2012 | 12.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| ellagic acid | | catechols;
cyclic ketone;
lactone;
organic heterotetracyclic compound;
polyphenol | antioxidant;
EC 1.14.18.1 (tyrosinase) inhibitor;
EC 2.3.1.5 (arylamine N-acetyltransferase) inhibitor;
EC 2.4.1.1 (glycogen phosphorylase) inhibitor;
EC 2.5.1.18 (glutathione transferase) inhibitor;
EC 2.7.1.127 (inositol-trisphosphate 3-kinase) inhibitor;
EC 2.7.1.151 (inositol-polyphosphate multikinase) inhibitor;
EC 2.7.4.6 (nucleoside-diphosphate kinase) inhibitor;
EC 2.7.7.7 (DNA-directed DNA polymerase) inhibitor;
EC 5.99.1.2 (DNA topoisomerase) inhibitor;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor;
food additive;
fungal metabolite;
geroprotector;
plant metabolite;
skin lightening agent | 2013 | 2013 | 11.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| sdz psc 833 | | homodetic cyclic peptide | | 2013 | 2021 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 1 |
| pitavastatin | | cyclopropanes;
dihydroxy monocarboxylic acid;
monofluorobenzenes;
quinolines;
statin (synthetic) | antioxidant | 2018 | 2018 | 6.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| neobavaisoflavone | | 7-hydroxyisoflavones | antineoplastic agent;
EC 2.7.7.7 (DNA-directed DNA polymerase) inhibitor;
plant metabolite;
platelet aggregation inhibitor | 2016 | 2016 | 8.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| demethoxycurcumin | | beta-diketone;
diarylheptanoid;
enone;
polyphenol | anti-inflammatory agent;
antineoplastic agent;
metabolite | 2019 | 2019 | 5.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| phytochlorin | | | | 2018 | 2018 | 6.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| 3,8-dihydroxy-6h-dibenzo(b,d)pyran-6-one | | coumarins | geroprotector | 2013 | 2013 | 11.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| 4,4'-diisothiocyanostilbene-2,2'-disulfonic acid | | | | 2016 | 2016 | 8.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| (3S,5S,6E)-7-[3-(4-fluorophenyl)-1-(propan-2-yl)-1H-indol-2-yl]-3,5-dihydroxyhept-6-enoic acid | | (6E)-7-[3-(4-fluorophenyl)-1-(propan-2-yl)-1H-indol-2-yl]-3,5-dihydroxyhept-6-enoic acid | | 2019 | 2019 | 5.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| verlukast | | | | 2009 | 2019 | 10.0 | medium | 0 | 0 | 0 | 2 | 12 | 0 |
| nitrofurantoin | | imidazolidine-2,4-dione;
nitrofuran antibiotic;
organonitrogen heterocyclic antibiotic;
organooxygen heterocyclic antibiotic | antibacterial drug;
antiinfective agent;
hepatotoxic agent | 2011 | 2011 | 13.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| rivaroxaban | | aromatic amide;
lactam;
monocarboxylic acid amide;
morpholines;
organochlorine compound;
oxazolidinone;
thiophenes | anticoagulant;
EC 3.4.21.6 (coagulation factor Xa) inhibitor | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| hypaconitine | | | | 2013 | 2013 | 11.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| apixaban | | aromatic ether;
lactam;
piperidones;
pyrazolopyridine | anticoagulant;
EC 3.4.21.6 (coagulation factor Xa) inhibitor | 2013 | 2013 | 11.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| regorafenib | | (trifluoromethyl)benzenes;
aromatic ether;
monochlorobenzenes;
monofluorobenzenes;
phenylureas;
pyridinecarboxamide | antineoplastic agent;
hepatotoxic agent;
tyrosine kinase inhibitor | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| chlorophyll a | | chlorophyll;
methyl ester | cofactor | 2010 | 2010 | 14.0 | low | 0 | 0 | 0 | 1 | 0 | 0 |
| hoe 33342 | | | | 2010 | 2021 | 8.3 | low | 0 | 0 | 0 | 1 | 1 | 1 |
| incb-018424 | | nitrile;
pyrazoles;
pyrrolopyrimidine | antineoplastic agent;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor | 2021 | 2021 | 3.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| yqa14 | | | | 2015 | 2015 | 9.0 | medium | 0 | 0 | 0 | 0 | 1 | 0 |
| novobiocin | | carbamate ester;
ether;
hexoside;
hydroxycoumarin;
monocarboxylic acid amide;
monosaccharide derivative;
phenols | antibacterial agent;
antimicrobial agent;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor;
Escherichia coli metabolite;
hepatoprotective agent | 2010 | 2010 | 14.0 | low | 0 | 0 | 0 | 1 | 0 | 0 |
| warfarin | | benzenes;
hydroxycoumarin;
methyl ketone | | 2013 | 2013 | 11.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| tridihexethyl | | | | 2013 | 2013 | 11.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| aconitine | | | | 2013 | 2013 | 11.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| cyclosporine | | | | 2013 | 2016 | 10.0 | low | 0 | 0 | 0 | 0 | 3 | 0 |
| dacarbazine | | dacarbazine | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| pyrimidinones | | | | 2008 | 2008 | 16.0 | low | 0 | 0 | 0 | 1 | 0 | 0 |
| Condition | Indicated | Studies | First Year | Last Year | Average Age | Relationship Strength | Trials | pre-1990 | 1990's | 2000's | 2010's | post-2020 |
|---|
| Airflow Obstruction, Chronic | 0 | | 2013 | 2013 | 11.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Animal Mammary Carcinoma | 0 | | 2012 | 2012 | 12.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Asthma | 0 | | 2013 | 2013 | 11.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Asthma, Bronchial | 0 | | 2013 | 2013 | 11.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Astrocytoma, Grade IV | 0 | | 2017 | 2022 | 5.0 | low | 0 | 0 | 0 | 0 | 2 | 1 |
| Benign Neoplasms | 0 | | 2008 | 2008 | 16.0 | low | 0 | 0 | 0 | 1 | 0 | 0 |
| Benign Neoplasms, Brain | 0 | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Brain Neoplasms | 0 | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Breast Cancer | 0 | | 2010 | 2019 | 9.2 | medium | 0 | 0 | 0 | 1 | 5 | 0 |
| Breast Neoplasms | 0 | | 2010 | 2019 | 9.2 | medium | 0 | 0 | 0 | 1 | 5 | 0 |
| Cancer of Colon | 0 | | 2012 | 2015 | 10.5 | low | 0 | 0 | 0 | 0 | 2 | 0 |
| Cancer of Gastrointestinal Tract | 0 | | 2019 | 2019 | 5.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Cancer of Liver | 0 | | 2021 | 2021 | 3.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| Cancer of Lung | 0 | | 2014 | 2014 | 10.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Carcinoma, Hepatocellular | 0 | | 2021 | 2021 | 3.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| Carcinoma, Non-Small Cell Lung | 0 | | 2014 | 2014 | 10.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Carcinoma, Non-Small-Cell Lung | 0 | | 2014 | 2014 | 10.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Cerebral Cryptococcosis | 0 | | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Colonic Neoplasms | 0 | | 2012 | 2015 | 10.5 | low | 0 | 0 | 0 | 0 | 2 | 0 |
| Disease Models, Animal | 0 | | 2015 | 2020 | 6.5 | low | 0 | 0 | 0 | 0 | 2 | 0 |
| ER-Negative PR-Negative HER2-Negative Breast Cancer | 0 | | 2015 | 2015 | 9.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Erythremia | 0 | | 2021 | 2021 | 3.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| Experimental Neoplasms | 0 | | 2013 | 2013 | 11.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Glioblastoma | 0 | | 2017 | 2022 | 5.0 | low | 0 | 0 | 0 | 0 | 2 | 1 |
| Hepatocellular Carcinoma | 0 | | 2021 | 2021 | 3.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| Injury, Ischemia-Reperfusion | 0 | | 2012 | 2012 | 12.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Liver Neoplasms | 0 | | 2021 | 2021 | 3.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| Lung Neoplasms | 0 | | 2014 | 2014 | 10.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Meningitis, Cryptococcal | 0 | | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Myeloproliferative Disorders | 0 | | 2021 | 2021 | 3.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| Neoplasms | 0 | | 2008 | 2008 | 16.0 | low | 0 | 0 | 0 | 1 | 0 | 0 |
| Polycythemia Vera | 0 | | 2021 | 2021 | 3.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| Pregnancy | 0 | | 2010 | 2018 | 10.0 | low | 0 | 0 | 0 | 1 | 1 | 0 |
| Pulmonary Disease, Chronic Obstructive | 0 | | 2013 | 2013 | 11.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Reperfusion Injury | 0 | | 2012 | 2012 | 12.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Triple Negative Breast Neoplasms | 0 | | 2015 | 2015 | 9.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
Fluorescence-based discrimination of breast cancer cells by direct exposure to 5-aminolevulinic acid.Cancer medicine, , Volume: 8, Issue:12, 2019
Involvement of the Transporters P-Glycoprotein and Breast Cancer Resistance Protein in Dermal Distribution of the Multikinase Inhibitor Regorafenib and Its Active Metabolites.Journal of pharmaceutical sciences, , Volume: 106, Issue:9, 2017
The linker region of breast cancer resistance protein ABCG2 is critical for coupling of ATP-dependent drug transport.Cellular and molecular life sciences : CMLS, , Volume: 73, Issue:9, 2016
Breast cancer resistance protein-mediated efflux of luteolin glucuronides in HeLa cells overexpressing UDP-glucuronosyltransferase 1A9.Pharmaceutical research, , Volume: 31, Issue:4, 2014
The gut microbiota ellagic acid-derived metabolite urolithin A and its sulfate conjugate are substrates for the drug efflux transporter breast cancer resistance protein (ABCG2/BCRP).Journal of agricultural and food chemistry, , May-08, Volume: 61, Issue:18, 2013
Specific inhibitors of the breast cancer resistance protein (BCRP).ChemMedChem, , Sep-03, Volume: 5, Issue:9, 2010
Ko143 Reverses MDR in Glioblastoma Anticancer research, , Volume: 42, Issue:2, 2022
ABCG2-mediated suppression of chlorin e6 accumulation and photodynamic therapy efficiency in glioblastoma cell lines can be reversed by KO143.Journal of photochemistry and photobiology. B, Biology, , Volume: 178, 2018
Expression and function of ABCG2 and XIAP in glioblastomas.Journal of neuro-oncology, , Volume: 133, Issue:1, 2017
Transport mechanism of ursodeoxycholic acid in human placental BeWo cells.Biopharmaceutics & drug disposition, , Volume: 39, Issue:7, 2018
Toxicokinetics of the food-toxin IQ in human placental perfusion is not affected by ABCG2 or xenobiotic metabolism.Placenta, , Volume: 31, Issue:7, 2010
Increase of the uterus-relaxant effect of nifedipine by the Abcg2 efflux protein inhibitor KO134 in the rat in vivo.In vivo (Athens, Greece), , Volume: 27, Issue:3
Fluorescence-based discrimination of breast cancer cells by direct exposure to 5-aminolevulinic acid.Cancer medicine, , Volume: 8, Issue:12, 2019
Involvement of the Transporters P-Glycoprotein and Breast Cancer Resistance Protein in Dermal Distribution of the Multikinase Inhibitor Regorafenib and Its Active Metabolites.Journal of pharmaceutical sciences, , Volume: 106, Issue:9, 2017
The linker region of breast cancer resistance protein ABCG2 is critical for coupling of ATP-dependent drug transport.Cellular and molecular life sciences : CMLS, , Volume: 73, Issue:9, 2016
Breast cancer resistance protein-mediated efflux of luteolin glucuronides in HeLa cells overexpressing UDP-glucuronosyltransferase 1A9.Pharmaceutical research, , Volume: 31, Issue:4, 2014
The gut microbiota ellagic acid-derived metabolite urolithin A and its sulfate conjugate are substrates for the drug efflux transporter breast cancer resistance protein (ABCG2/BCRP).Journal of agricultural and food chemistry, , May-08, Volume: 61, Issue:18, 2013
Specific inhibitors of the breast cancer resistance protein (BCRP).ChemMedChem, , Sep-03, Volume: 5, Issue:9, 2010
Ko143 Reverses MDR in Glioblastoma Anticancer research, , Volume: 42, Issue:2, 2022
ABCG2-mediated suppression of chlorin e6 accumulation and photodynamic therapy efficiency in glioblastoma cell lines can be reversed by KO143.Journal of photochemistry and photobiology. B, Biology, , Volume: 178, 2018
Expression and function of ABCG2 and XIAP in glioblastomas.Journal of neuro-oncology, , Volume: 133, Issue:1, 2017
Pharmacokinetics (1)
Bioavailability (8)
| Article | Year |
|---|
Mechanism of the efflux transport of demethoxycurcumin-O-glucuronides in HeLa cells stably transfected with UDP-glucuronosyltransferase 1A1.
PloS one, , Volume: 14, Issue:5 | 2019 |
Synthesis of a new inhibitor of breast cancer resistance protein with significantly improved pharmacokinetic profiles.
Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 26, Issue:2 | 2016 |
Efflux and uptake transporters involved in the disposition of bazedoxifene.
European journal of drug metabolism and pharmacokinetics, , Volume: 41, Issue:3 | 2016 |
In vivo assessment of the impact of efflux transporter on oral drug absorption using portal vein-cannulated rats.
Drug metabolism and disposition: the biological fate of chemicals, , Volume: 41, Issue:8 | 2013 |
Evaluation of intestinal absorption of amtolmetin guacyl in rats: breast cancer resistant protein as a primary barrier of oral bioavailability.
Life sciences, , Feb-27, Volume: 92, Issue:3 | 2013 |
Breast cancer resistance protein (ABCG2) determines distribution of genistein phase II metabolites: reevaluation of the roles of ABCG2 in the disposition of genistein.
Drug metabolism and disposition: the biological fate of chemicals, , Volume: 40, Issue:10 | 2012 |
Assessment and modulation of forsythiaside absorption with MDCKII cells and validation with in situ intestinal experiment.
European journal of drug metabolism and pharmacokinetics, , Volume: 37, Issue:3 | 2012 |
Interaction of gatifloxacin with efflux transporters: a possible mechanism for drug resistance.
International journal of pharmaceutics, , Aug-16, Volume: 395, Issue:1-2 | 2010 |