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Literature summary for 2.4.1.17 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)

Cloned (Comment) Organism
-
Homo sapiens

Inhibitors

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

KM Value [mM]

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

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

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

IC50 Value

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