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 (Comment) | Organism |
---|---|
expressed in HEK-293T cells | Homo sapiens |
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 | Comment | Organism | GeneOntology No. | Textmining |
---|---|---|---|---|
microsome | - |
Homo sapiens | - |
- |
Metals/Ions | Comment | Organism | Structure |
---|---|---|---|
Mg2+ | 4 mM used in assay conditions | Homo sapiens |
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 | Comment | Organism | Textmining |
---|---|---|---|
liver | - |
Homo sapiens | - |
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 | 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 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 |