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Literature summary for 2.4.1.17 extracted from

  • Wang, F.; Wang, S.; Yang, K.; Liu, Y.Z.; Yang, K.; Chen, Y.; Fang, Z.Z.
    Inhibition of UDP-glucuronosyltransferases (UGTs) by bromophenols (BPs) (2020), Chemosphere, 238, 124645 .
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
2,4,6-tribromophenol competitive inhibition; competitive inhibition; competitive inhibition; noncompetitive inhibition Homo sapiens
2,4-Dibromophenol competitive inhibition; competitive inhibition; competitive inhibition; competitive inhibition Homo sapiens
2,5-dibromophenol competitive inhibition; competitive inhibition; competitive inhibition; competitive inhibition Homo sapiens
2-bromophenol competitive inhibition; competitive inhibition Homo sapiens
3,5-dibromophenol competitive inhibition; competitive inhibition; competitive inhibition; competitive inhibition Homo sapiens
additional information not inhibited by 2,4-dibromophenol, 2,5-dibromophenol and 2,4,6-tribromophenol; not inhibited by 2-bromophenol; not inhibited by 2-bromophenol, 2,4-dibromophenol, 2,5-dibromophenol and 2,4,6-tribromophenol; not inhibited by 2-bromophenol, 2,4-dibromophenol, 2,5-dibromophenol and 3,5-dibromophenol; not inhibited by 2-bromophenol, 2,4-dibromophenol, 3,5-dibromophenol and 2,4,6-tribromophenol; not inhibited by 2-bromophenol and 2,4,6-tribromophenol; not inhibited by 2-bromophenol and 2,4-dibromophenol Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens O60656
-
-
Homo sapiens P16662
-
-
Homo sapiens P19224
-
-
Homo sapiens P22309
-
-
Homo sapiens P35503
-
-
Homo sapiens Q9HAW7
-
-
Homo sapiens Q9HAW9
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
4-methylumbelliferone + UDP-glucuronate
-
Homo sapiens UDP + 4-methylumbelliferyl beta-D-glucuronide
-
?

Synonyms

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

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.00002
-
2,5-dibromophenol isoform UGT2B7, at pH 7.4 and 37°C Homo sapiens
0.00048
-
3,5-dibromophenol isoform UGT2B7, at pH 7.4 and 37°C Homo sapiens
0.00094
-
2,5-dibromophenol isoform UGT1A1, at pH 7.4 and 37°C Homo sapiens
0.00095
-
2,5-dibromophenol isoform UGT1A9, at pH 7.4 and 37°C Homo sapiens
0.00146
-
2,4-Dibromophenol isoform UGT1A7, at pH 7.4 and 37°C Homo sapiens
0.00156
-
2,5-dibromophenol isoform UGT1A7, at pH 7.4 and 37°C Homo sapiens
0.00174
-
2-bromophenol isoform UGT1A6, at pH 7.4 and 37°C Homo sapiens
0.00246
-
3,5-dibromophenol isoform UGT1A6, at pH 7.4 and 37°C Homo sapiens
0.00285
-
2,4,6-tribromophenol isoform UGT1A3, at pH 7.4 and 37°C Homo sapiens
0.00372
-
2,4-Dibromophenol isoform UGT1A9, at pH 7.4 and 37°C Homo sapiens
0.00399
-
2,4,6-tribromophenol isoform UGT1A7, at pH 7.4 and 37°C Homo sapiens
0.031
-
2,4,6-tribromophenol isoform UGT2B7, at pH 7.4 and 37°C Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00013
-
isoform UGT1A7, at pH 7.4 and 37°C Homo sapiens 2,4-Dibromophenol
0.00014
-
isoform UGT2B7, at pH 7.4 and 37°C Homo sapiens 2,5-dibromophenol
0.00015
-
isoform UGT1A9, at pH 7.4 and 37°C Homo sapiens 2,5-dibromophenol
0.00018
-
isoform UGT1A9, at pH 7.4 and 37°C Homo sapiens 3,5-dibromophenol
0.00022
-
isoform UGT1A9, at pH 7.4 and 37°C Homo sapiens 2,4-Dibromophenol
0.00058
-
isoform UGT1A6, at pH 7.4 and 37°C Homo sapiens 3,5-dibromophenol
0.00062
-
isoform UGT1A7, at pH 7.4 and 37°C Homo sapiens 2,5-dibromophenol
0.00064
-
isoform UGT1A7, at pH 7.4 and 37°C Homo sapiens 2,4,6-tribromophenol
0.0019
-
isoform UGT1A6, at pH 7.4 and 37°C Homo sapiens 2-bromophenol
0.00193
-
isoform UGT2B7, at pH 7.4 and 37°C Homo sapiens 3,5-dibromophenol
0.00507
-
isoform UGT1A1, at pH 7.4 and 37°C Homo sapiens 2,5-dibromophenol
0.00747
-
isoform UGT1A3, at pH 7.4 and 37°C Homo sapiens 2,4,6-tribromophenol
0.00858
-
isoform UGT2B7, at pH 7.4 and 37°C Homo sapiens 2,4,6-tribromophenol
0.01
-
isoform UGT1A7, at pH 7.4 and 37°C Homo sapiens 3,5-dibromophenol