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Literature summary extracted from

  • Murakami, M.; Ohnuma, S.; Fukuda, M.; Chufan, E.E.; Kudoh, K.; Kanehara, K.; Sugisawa, N.; Ishida, M.; Naitoh, T.; Shibata, H.; Iwabuchi, Y.; Ambudkar, S.V.; Unno, M.
    Synthetic analogs of curcumin modulate the function of multidrug resistance-linked ATP-binding cassette transporter ABCG2 (2017), Drug Metab. Dispos., 45, 1166-1177 .
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

EC Number Cloned (Comment) Organism
7.6.2.2 expressed in High Five insect cells Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
7.6.2.2 (1E)-1,5-bis[3,5-bis(methoxymethoxy)phenyl]-4,4-dibromopent-1-en-3-one 58.7% inhibition at 0.01 mM Homo sapiens
7.6.2.2 (1E)-1,5-bis[3,5-bis(methoxymethoxy)phenyl]-4,4-dichloropent-1-en-3-one 51.5% inhibition at 0.01 mM Homo sapiens
7.6.2.2 (1E)-1,5-bis[3,5-bis(methoxymethoxy)phenyl]-4,4-difluoropent-1-en-3-one 44.4% inhibition at 0.01 mM Homo sapiens
7.6.2.2 (1E)-1-[3,5-bis(methoxymethoxy)phenyl]-4,4-dimethylpent-1-en-3-one 14.9% inhibition at 0.01 mM Homo sapiens
7.6.2.2 (1E,4E)-1,5-bis(4-hydroxy-3-methoxyphenyl)penta-1,4-dien-3-one 51.8% inhibition at 0.01 mM Homo sapiens
7.6.2.2 (1E,4E)-1,5-bis[3,4-bis(methoxymethoxy)phenyl]penta-1,4-dien-3-one 84.3% inhibition at 0.01 mM Homo sapiens
7.6.2.2 (1E,4E)-1-(2H-1,3-benzodioxol-5-yl)-5-[3,5-bis(methoxymethoxy)phenyl]penta-1,4-dien-3-one 57.4% inhibition at 0.01 mM Homo sapiens
7.6.2.2 (1E,4E)-1-(4-hydroxy-3,5-dimethoxyphenyl)-5-(3,4,5-trimethoxyphenyl)penta-1,4-dien-3-one 82.9% inhibition at 0.01 mM Homo sapiens
7.6.2.2 (1Z,4E)-1,5-bis[3,5-bis(methoxymethoxy)phenyl]-2-chloropenta-1,4-dien-3-one 83.2% inhibition at 0.01 mM Homo sapiens
7.6.2.2 (1Z,4E)-5-[3,5-bis(methoxymethoxy)phenyl]-2-bromo-1-[2-bromo-3,5-bis(methoxymethoxy)phenyl]penta-1,4-dien-3-one 77.4% inhibition at 0.01 mM Homo sapiens
7.6.2.2 (2E)-3-[3,5-bis(methoxymethoxy)phenyl]-N-methylprop-2-enamide 6.1% inhibition at 0.01 mM Homo sapiens
7.6.2.2 (2E)-3-[3,5-bis(methoxymethoxy)phenyl]prop-2-enal 9.2% inhibition at 0.01 mM Homo sapiens
7.6.2.2 (2E)-3-[3,5-bis(methoxymethoxy)phenyl]prop-2-enoic acid 0.3% inhibition at 0.01 mM Homo sapiens
7.6.2.2 (2E,6E)-2,6-bis[(2-fluorophenyl)methylidene]cyclohexan-1-one 30.5% inhibition at 0.01 mM Homo sapiens
7.6.2.2 (2E,6E)-2,6-bis[[3,5-bis(methoxymethoxy)phenyl]methylidene]cyclohexan-1-one 69.8% inhibition at 0.01 mM Homo sapiens
7.6.2.2 (3E,5E)-3,5-bis[[3,5-bis(methoxymethoxy)phenyl]methylidene]-1-methylpiperidin-4-one 52% inhibition at 0.01 mM Homo sapiens
7.6.2.2 (4E)-5-[3,5-bis(methoxymethoxy)phenyl]-2-[[3,4-bis(methoxymethoxy)phenyl]methyl]-3-oxopent-4-enenitrile 29.9% inhibition at 0.01 mM Homo sapiens
7.6.2.2 1,5-bis[3,4-bis(methoxymethoxy)phenyl]-1,5-bis(phenylsulfanyl)pentan-3-one 26.6% inhibition at 0.01 mM Homo sapiens
7.6.2.2 1,5-bis[3,4-bis(methoxymethoxy)phenyl]-1,5-bis[(2,3-dihydroxypropyl)sulfanyl]pentan-3-one 1.6% inhibition at 0.01 mM Homo sapiens
7.6.2.2 1,5-bis[3,5-bis(methoxymethoxy)phenyl]-1,5-bis(ethylsulfanyl)pentan-3-one 37.1% inhibition at 0.01 mM Homo sapiens
7.6.2.2 curcumin 99.5% inhibition at 0.01 mM Homo sapiens
7.6.2.2 Kol43
-
 Homo sapiens
7.6.2.2 methyl (2E)-3-[3,5-bis(methoxymethoxy)phenyl]prop-2-enoate 8.6% inhibition at 0.01 mM Homo sapiens
7.6.2.2 N,N'-[[1,5-bis[3,4-bis(methoxymethoxy)phenyl]-3-oxopentane-1,5-diyl]bis(sulfanediylethane-2,1-diyl)]diacetamide 15.2% inhibition at 0.01 mM Homo sapiens
7.6.2.2 S-propyl (2E)-3-[3,5-bis(methoxymethoxy)phenyl]prop-2-enethioate 28.2% inhibition at 0.01 mM Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
7.6.2.2 ATP + H2O + xenobiotic[side 1] Homo sapiens
-
 ADP + phosphate + xenobiotic[side 2]
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
7.6.2.2 Homo sapiens Q9UNQ0
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
7.6.2.2 K-562 cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
7.6.2.2 ATP + H2O + iodoarylazidoprazosin[side 1]
-
 Homo sapiens ADP + phosphate + iodoarylazidoprazosin[side 2]
-
 ?
7.6.2.2 ATP + H2O + mitoxantrone[side 1]
-
 Homo sapiens ADP + phosphate + mitoxantrone[side 2]
-
 ?
7.6.2.2 ATP + H2O + pheophorbide A[side 1]
-
 Homo sapiens ADP + phosphate + pheophorbide A[side 2]
-
 ?
7.6.2.2 ATP + H2O + SN-38[side 1] SN-38 is 7-ethyl-10-hydroxy-CPT Homo sapiens ADP + phosphate + SN-38[side 2]
-
 ?
7.6.2.2 ATP + H2O + xenobiotic[side 1]
-
 Homo sapiens ADP + phosphate + xenobiotic[side 2]
-
 ?

Synonyms

EC Number Synonyms Comment Organism
7.6.2.2 ABCG2
-
 Homo sapiens
7.6.2.2 BCRP
-
 Homo sapiens
7.6.2.2 breast cancer resistance protein
-
 Homo sapiens
7.6.2.2 multidrug resistance-linked ATP-binding cassette transporter
-
 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
7.6.2.2 0.00019
-
 at 37°C, pH not specified in the publication Homo sapiens Kol43
7.6.2.2 0.00025
-
 at 37°C, pH not specified in the publication Homo sapiens (1Z,4E)-1,5-bis[3,5-bis(methoxymethoxy)phenyl]-2-chloropenta-1,4-dien-3-one
7.6.2.2 0.00031
-
 at 37°C, pH not specified in the publication Homo sapiens (1E,4E)-1-(4-hydroxy-3,5-dimethoxyphenyl)-5-(3,4,5-trimethoxyphenyl)penta-1,4-dien-3-one
7.6.2.2 0.00037
-
 at 37°C, pH not specified in the publication Homo sapiens (1Z,4E)-5-[3,5-bis(methoxymethoxy)phenyl]-2-bromo-1-[2-bromo-3,5-bis(methoxymethoxy)phenyl]penta-1,4-dien-3-one
7.6.2.2 0.00051
-
 at 37°C, pH not specified in the publication Homo sapiens (1E,4E)-1,5-bis[3,4-bis(methoxymethoxy)phenyl]penta-1,4-dien-3-one
7.6.2.2 0.00062
-
 at 37°C, pH not specified in the publication Homo sapiens curcumin