Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary extracted from

  • Liu, Y.; She, M.; Wu, Z.; Dai, R.
    The inhibition study of human UDP-glucuronosyltransferases with cytochrome P450 selective substrates and inhibitors (2011), J. Enzyme Inhib. Med. Chem., 26, 386-393.
    View publication on PubMed

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.4.1.17
-
Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.4.1.17 2-phenyl-4H-benzo[h]chromen-4-one
-
Homo sapiens
2.4.1.17 bupropion
-
Homo sapiens
2.4.1.17 cyclosporine A
-
Homo sapiens
2.4.1.17 dextromethorphan
-
Homo sapiens
2.4.1.17 diclofenac
-
Homo sapiens
2.4.1.17 ketoconazole
-
Homo sapiens
2.4.1.17 midazolam
-
Homo sapiens
2.4.1.17 oleandomycin
-
Homo sapiens
2.4.1.17 Omeprazole
-
Homo sapiens
2.4.1.17 paclitaxel
-
Homo sapiens
2.4.1.17 quinidine
-
Homo sapiens
2.4.1.17 testosterone
-
Homo sapiens
2.4.1.17 Tolbutamide
-
Homo sapiens

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
2.4.1.17 0.013
-
midazolam isoform UGT1A4, pH 7.4, 37°C Homo sapiens
2.4.1.17 0.021
-
beta-estradiol isoform UGT1A1, pH 7.4, 37°C Homo sapiens
2.4.1.17 0.056
-
diclofenac isoform UGT2B10, pH 7.4, 37°C Homo sapiens
2.4.1.17 0.069
-
diclofenac isoform UGT2B7, pH 7.4, 37°C Homo sapiens
2.4.1.17 0.084
-
1-naphthol isoform UGT1A6, pH 7.4, 37°C Homo sapiens

Organism

EC Number Organism UniProt Comment Textmining
2.4.1.17 Homo sapiens
-
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.4.1.17 1-naphthol + UDP-alpha-D-glucuronate
-
Homo sapiens 1-naphthyl-O-glucuronide + UDP
-
?
2.4.1.17 beta-estradiol + UDP-alpha-D-glucuronate
-
Homo sapiens beta-estradiol-3-glucuronide + UDP
-
?
2.4.1.17 diclofenac + UDP-alpha-D-glucuronate
-
Homo sapiens diclofenac D-glucuronide + UDP
-
?
2.4.1.17 midazolam + UDP-alpha-D-glucuronate
-
Homo sapiens midazolam D-glucuronide + UDP
-
?

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.4.1.17 0.0041
-
isoform UGT1A1, substrate beta-estradiol, pH 7.4, 37°C Homo sapiens ketoconazole
2.4.1.17 0.0049
-
isoform UGT1A4, substrate midazolam, pH 7.4, 37°C Homo sapiens paclitaxel
2.4.1.17 0.019
-
isoform UGT1A6, substrate 1-naphthol, pH 7.4, 37°C Homo sapiens ketoconazole
2.4.1.17 0.02
-
isoform UGT1A1, substrate beta-estradiol, pH 7.4, 37°C Homo sapiens paclitaxel
2.4.1.17 0.022
-
isoform UGT2B10, substrate diclofenacl, pH 7.4, 37°C Homo sapiens ketoconazole
2.4.1.17 0.023
-
isoform UGT1A4, substrate midazolam, pH 7.4, 37°C Homo sapiens cyclosporine A
2.4.1.17 0.023
-
isoform UGT1A4, substrate midazolam, pH 7.4, 37°C Homo sapiens 2-phenyl-4H-benzo[h]chromen-4-one
2.4.1.17 0.023
-
isoform UGT1A6, substrate 1-naphthol, pH 7.4, 37°C Homo sapiens midazolam
2.4.1.17 0.026
-
isoform UGT1A1, substrate beta-estradiol, pH 7.4, 37°C Homo sapiens midazolam
2.4.1.17 0.038
-
isoform UGT1A1, substrate beta-estradiol, pH 7.4, 37°C Homo sapiens 2-phenyl-4H-benzo[h]chromen-4-one
2.4.1.17 0.043
-
isoform UGT1A1, substrate beta-estradiol, pH 7.4, 37°C Homo sapiens testosterone
2.4.1.17 0.044
-
isoform UGT1A1, substrate beta-estradiol, pH 7.4, 37°C Homo sapiens oleandomycin
2.4.1.17 0.046
-
isoform UGT1A4, substrate midazolam, pH 7.4, 37°C Homo sapiens diclofenac
2.4.1.17 0.048
-
isoform UGT1A1, substrate beta-estradiol, pH 7.4, 37°C Homo sapiens cyclosporine A
2.4.1.17 0.056
-
isoform UGT1A1, substrate beta-estradiol, pH 7.4, 37°C Homo sapiens Omeprazole
2.4.1.17 0.058
-
isoform UGT1A4, substrate midazolam, pH 7.4, 37°C Homo sapiens ketoconazole
2.4.1.17 0.059
-
isoform UGT1A4, substrate midazolam, pH 7.4, 37°C Homo sapiens oleandomycin
2.4.1.17 0.06
-
isoform UGT2B7, substrate diclofenac, pH 7.4, 37°C Homo sapiens ketoconazole
2.4.1.17 0.062
-
isoform UGT2B10, substrate diclofenac, pH 7.4, 37°C Homo sapiens dextromethorphan
2.4.1.17 0.067
-
isoform UGT1A6, substrate 1-naphthol, pH 7.4, 37°C Homo sapiens 2-phenyl-4H-benzo[h]chromen-4-one
2.4.1.17 0.074
-
isoform UGT1A6, substrate 1-naphthol, pH 7.4, 37°C Homo sapiens paclitaxel
2.4.1.17 0.088
-
isoform UGT2B10, substrate diclofenacl, pH 7.4, 37°C Homo sapiens bupropion
2.4.1.17 0.089
-
isoform UGT1A4, substrate midazolam, pH 7.4, 37°C Homo sapiens dextromethorphan
2.4.1.17 0.106
-
isoform UGT2B10, substrate diclofenacl, pH 7.4, 37°C Homo sapiens midazolam
2.4.1.17 0.147
-
isoform UGT2B7, substrate diclofenac, pH 7.4, 37°C Homo sapiens midazolam
2.4.1.17 0.149
-
isoform UGT2B7, substrate diclofenac, pH 7.4, 37°C Homo sapiens 2-phenyl-4H-benzo[h]chromen-4-one
2.4.1.17 0.152
-
isoform UGT1A4, substrate midazolam, pH 7.4, 37°C Homo sapiens bupropion
2.4.1.17 0.155
-
isoform UGT1A1, substrate beta-estradiol, pH 7.4, 37°C Homo sapiens diclofenac
2.4.1.17 0.165
-
isoform UGT2B7, substrate diclofenac, pH 7.4, 37°C Homo sapiens testosterone
2.4.1.17 0.166
-
isoform UGT1A4, substrate midazolam, pH 7.4, 37°C Homo sapiens quinidine
2.4.1.17 0.185
-
isoform UGT1A6, substrate 1-naphthol, pH 7.4, 37°C Homo sapiens Omeprazole
2.4.1.17 0.192
-
isoform UGT1A4, substrate midazolam, pH 7.4, 37°C Homo sapiens diclofenac
2.4.1.17 0.272
-
isoform UGT1A1, substrate beta-estradiol, pH 7.4, 37°C Homo sapiens oleandomycin
2.4.1.17 0.281
-
isoform UGT1A6, substrate 1-naphthol, pH 7.4, 37°C Homo sapiens Tolbutamide