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Literature summary for 2.4.1.17 extracted from

  • Korprasertthaworn, P.; Chau, N.; Nair, P.; Rowland, A.; Miners, J.
    Inhibition of human UDP-glucuronosyltransferase (UGT) enzymes by kinase inhibitors Effects of dabrafenib, ibrutinib, nintedanib, trametinib and BIBF 1202 (2019), Biochem. Pharmacol., 169, 113616 .
    View publication on PubMed
Search for more literature for 2.4.1.17

Activating Compound

Activating Compound Comment Organism Structure
BIBF 1202 100% activity at 0.05 mM Homo sapiens
BIBF 1202 105% activity at 0.01 mM Homo sapiens
ibrutinib about 130% activity at 0.05 mM Homo sapiens
nintedanib about 105% activity at 0.01 mM Homo sapiens
nintedanib about 105% activity at 0.05 mM Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
expressed in HEK-293T cells Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
BIBF 1202 about 60% residual activity at 0.05 mM; about 70% residual activity at 0.05 mM; about 75% residual activity at 0.05 mM; about 75% residual activity at 0.05 mM; about 75% residual activity at 0.05 mM; about 85% residual activity at 0.05 mM; about 85% residual activity at 0.05 mM; about 87% residual activity at 0.05 mM; about 90% residual activity at 0.05 mM; about 90% residual activity at 0.05 mM Homo sapiens
dabrafenib about 10% residual activity at 0.05 mM; about 17% residual activity at 0.05 mM; about 30% residual activity at 0.05 mM; about 38% residual activity at 0.05 mM; about 40% residual activity at 0.05 mM; about 40% residual activity at 0.05 mM; about 55% residual activity at 0.05 mM; about 59% residual activity at 0.05 mM; about 5% residual activity at 0.05 mM; about 68% residual activity at 0.05 mM; about 8% residual activity at 0.05 mM; about 8% residual activity at 0.05 mM Homo sapiens
ibrutinib about 12% residual activity at 0.05 mM; about 12% residual activity at 0.05 mM; about 12% residual activity at 0.05 mM; about 20% residual activity at 0.05 mM; about 20% residual activity at 0.05 mM; about 20% residual activity at 0.05 mM; about 25% residual activity at 0.05 mM; about 2% residual activity at 0.05 mM; about 50% residual activity at 0.05 mM; about 5% residual activity at 0.05 mM; about 5% residual activity at 0.05 mM Homo sapiens
nintedanib about 10% residual activity at 0.05 mM; about 15% residual activity at 0.05 mM; about 18% residual activity at 0.05 mM; about 1% residual activity at 0.05 mM; about 25% residual activity at 0.05 mM; about 38% residual activity at 0.05 mM; about 3% residual activity at 0.05 mM; about 40% residual activity at 0.05 mM; about 5% residual activity at 0.05 mM; about 5% residual activity at 0.05 mM Homo sapiens
trametinib about 10% residual activity at 0.05 mM; about 25% residual activity at 0.05 mM; about 25% residual activity at 0.05 mM; about 25% residual activity at 0.05 mM; about 2% residual activity at 0.05 mM; about 30% residual activity at 0.05 mM; about 45% residual activity at 0.05 mM; about 45% residual activity at 0.05 mM; about 5% residual activity at 0.05 mM; about 60% residual activity at 0.05 mM; about 6% residual activity at 0.05 mM; about 85% residual activity at 0.05 mM Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
microsome
-
 Homo sapiens
-
-

Metals/Ions

Metals/Ions Comment Organism Structure
Mg2+ 4 mM used in assay conditions Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens A0A0G2JMZ5
-
-
Homo sapiens D6RH08
-
-
Homo sapiens O60656
-
-
Homo sapiens P06133
-
-
Homo sapiens P16662
-
-
Homo sapiens P19224
-
-
Homo sapiens P22309
-
-
Homo sapiens P22310
-
-
Homo sapiens P35503
-
-
Homo sapiens Q9HAW7
-
-
Homo sapiens Q9HAW8
-
-
Homo sapiens Q9HAW9
-
-

Source Tissue

Source Tissue Comment Organism Textmining
liver
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
beta-estradiol + UDP-glucuronate
-
 Homo sapiens UDP + beta-estradiol 3-O-glucuronide
-
 ?
propofol + UDP-glucuronate
-
 Homo sapiens UDP + propofol beta-D-glucuronoside
-
 ?
trifluoperazine + UDP-glucuronate
-
 Homo sapiens UDP + trifluoperazine beta-D-glucuronoside
-
 ?

Synonyms

Synonyms Comment Organism
UDP-glucuronosyltransferase
-
 Homo sapiens
UGT1A1 isoform Homo sapiens
UGT1A10 isoform Homo sapiens
UGT1A3 isoform Homo sapiens
UGT1A4 isoform Homo sapiens
UGT1A6 isoform Homo sapiens
UGT1A7 isoform Homo sapiens
UGT1A8 isoform Homo sapiens
UGT1A9 isoform Homo sapiens
UGT2B15 isoform Homo sapiens
UGT2B4 isoform Homo sapiens
UGT2B7 isoform Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0005
-
 isoform UGT1A9, at pH 7.4, temperature not specified in the publication Homo sapiens nintedanib
0.0007
-
 isoform UGT1A7, at pH 7.4, temperature not specified in the publication Homo sapiens ibrutinib
0.0009
-
 isoform UGT1A8, at pH 7.4, temperature not specified in the publication Homo sapiens ibrutinib
0.0011
-
 isoform UGT1A4, at pH 7.4, temperature not specified in the publication Homo sapiens trametinib
0.0013
-
 isoform UGT1A1, at pH 7.4, temperature not specified in the publication Homo sapiens trametinib
0.0014
-
 isoform UGT1A1, at pH 7.4, temperature not specified in the publication Homo sapiens ibrutinib
0.0019
-
 isoform UGT1A10, at pH 7.4, temperature not specified in the publication Homo sapiens trametinib
0.002
-
 isoform UGT1A7, at pH 7.4, temperature not specified in the publication Homo sapiens nintedanib
0.0022
-
 isoform UGT1A7, at pH 7.4, temperature not specified in the publication Homo sapiens dabrafenib
0.0023
-
 isoform UGT1A10, at pH 7.4, temperature not specified in the publication Homo sapiens nintedanib
0.0027
-
 isoform UGT1A8, at pH 7.4, temperature not specified in the publication Homo sapiens nintedanib
0.0028
-
 isoform UGT1A1, at pH 7.4, temperature not specified in the publication Homo sapiens nintedanib
0.0037
-
 isoform UGT1A10, at pH 7.4, temperature not specified in the publication Homo sapiens ibrutinib
0.0043
-
 isoform UGT2B15, at pH 7.4, temperature not specified in the publication Homo sapiens ibrutinib
0.00441
-
 isoform UGT1A8, at pH 7.4, temperature not specified in the publication Homo sapiens dabrafenib
0.0048
-
 isoform UGT1A10, at pH 7.4, temperature not specified in the publication Homo sapiens dabrafenib
0.0048
-
 isoform UGT1A9, at pH 7.4, temperature not specified in the publication Homo sapiens dabrafenib
0.0059
-
 isoform UGT1A3, at pH 7.4, temperature not specified in the publication Homo sapiens ibrutinib
0.0088
-
 isoform UGT1A1, at pH 7.4, temperature not specified in the publication Homo sapiens dabrafenib
0.009
-
 isoform UGT2B7, at pH 7.4, temperature not specified in the publication Homo sapiens nintedanib
0.0095
-
 isoform UGT1A9, at pH 7.4, temperature not specified in the publication Homo sapiens ibrutinib
0.012
-
 isoform UGT2B7, at pH 7.4, temperature not specified in the publication Homo sapiens ibrutinib
0.013
-
 isoform UGT2B7, at pH 7.4, temperature not specified in the publication Homo sapiens ibrutinib
0.016
-
 isoform UGT1A7, at pH 7.4, temperature not specified in the publication Homo sapiens trametinib
0.016
-
 isoform UGT2B7, at pH 7.4, temperature not specified in the publication Homo sapiens trametinib
0.016
-
 isoform UGT2B7, at pH 7.4, temperature not specified in the publication Homo sapiens nintedanib
0.018
-
 isoform UGT2B15, at pH 7.4, temperature not specified in the publication Homo sapiens nintedanib
0.023
-
 isoform UGT1A3, at pH 7.4, temperature not specified in the publication Homo sapiens trametinib
0.023
-
 isoform UGT2B7, at pH 7.4, temperature not specified in the publication Homo sapiens trametinib
0.027
-
 isoform UGT1A4, at pH 7.4, temperature not specified in the publication Homo sapiens nintedanib
0.029
-
 isoform UGT2B15, at pH 7.4, temperature not specified in the publication Homo sapiens dabrafenib
0.031
-
 isoform UGT1A6, at pH 7.4, temperature not specified in the publication Homo sapiens ibrutinib
0.036
-
 isoform UGT2B15, at pH 7.4, temperature not specified in the publication Homo sapiens trametinib
0.038
-
 isoform UGT1A6, at pH 7.4, temperature not specified in the publication Homo sapiens dabrafenib
0.039
-
 isoform UGT1A9, at pH 7.4, temperature not specified in the publication Homo sapiens trametinib
0.039
-
 isoform UGT2B7, at pH 7.4, temperature not specified in the publication Homo sapiens dabrafenib
0.04
-
 isoform UGT2B4, at pH 7.4, temperature not specified in the publication Homo sapiens dabrafenib
0.054
-
 isoform UGT1A6, at pH 7.4, temperature not specified in the publication Homo sapiens trametinib
0.059
-
 isoform UGT1A6, at pH 7.4, temperature not specified in the publication Homo sapiens nintedanib
0.07
-
 isoform UGT2B7, at pH 7.4, temperature not specified in the publication Homo sapiens dabrafenib
0.083
-
 isoform UGT2B4, at pH 7.4, temperature not specified in the publication Homo sapiens ibrutinib
0.09
-
 isoform UGT1A8, at pH 7.4, temperature not specified in the publication Homo sapiens trametinib
0.094
-
 isoform UGT1A4, at pH 7.4, temperature not specified in the publication Homo sapiens dabrafenib
0.1
-
 IC50 above 0.1 mM, isoform UGT1A1, at pH 7.4, temperature not specified in the publication Homo sapiens BIBF 1202
0.1
-
 IC50 above 0.1 mM, isoform UGT1A10, at pH 7.4, temperature not specified in the publication Homo sapiens BIBF 1202
0.1
-
 IC50 above 0.1 mM, isoform UGT1A3, at pH 7.4, temperature not specified in the publication Homo sapiens dabrafenib
0.1
-
 IC50 above 0.1 mM, isoform UGT1A3, at pH 7.4, temperature not specified in the publication Homo sapiens BIBF 1202
0.1
-
 IC50 above 0.1 mM, isoform UGT1A4, at pH 7.4, temperature not specified in the publication Homo sapiens BIBF 1202
0.1
-
 IC50 above 0.1 mM, isoform UGT1A7, at pH 7.4, temperature not specified in the publication Homo sapiens BIBF 1202
0.1
-
 IC50 above 0.1 mM, isoform UGT1A8, at pH 7.4, temperature not specified in the publication Homo sapiens BIBF 1202
0.1
-
 IC50 above 0.1 mM, isoform UGT1A9, at pH 7.4, temperature not specified in the publication Homo sapiens BIBF 1202
0.1
-
 IC50 above 0.1 mM, isoform UGT2B15, at pH 7.4, temperature not specified in the publication Homo sapiens BIBF 1202
0.1
-
 IC50 above 0.1 mM, isoform UGT2B4, at pH 7.4, temperature not specified in the publication Homo sapiens trametinib
0.1
-
 IC50 above 0.1 mM, isoform UGT2B4, at pH 7.4, temperature not specified in the publication Homo sapiens BIBF 1202
0.1
-
 IC50 above 0.1 mM, isoform UGT2B7, at pH 7.4, temperature not specified in the publication Homo sapiens BIBF 1202
0.18
-
 IC50 above 0.1 mM, isoform UGT2B41, at pH 7.4, temperature not specified in the publication Homo sapiens nintedanib