General Information of the Protein
Protein ID
PT02311
Protein Name
UDP-glucuronosyltransferase 1A1
Secondarily
Protein Name
Bilirubin-specific UDPGT isozyme 1
UDP-glucuronosyltransferase 1-1
UDP-glucuronosyltransferase 1A isoform 1
Gene Name
UGT1A1
Secondarily
Gene Name
GNT1
UGT1
Sequence
MAVESQGGRPLVLGLLLCVLGPVVSHAGKILLIPVDGSHWLSMLGAIQQLQQRGHEIVVLAPDASLYIRDGAFYTLKTYPVPFQREDVKESFVSLGHNVFENDSFLQRVIKTYKKIKKDSAMLLSGCSHLLHNKELMASLAESSFDVMLTDPFLPCSPIVAQYLSLPTVFFLHALPCSLEFEATQCPNPFSYVPRPLSSHSDHMTFLQRVKNMLIAFSQNFLCDVVYSPYATLASEFLQREVTVQDLLSSASVWLFRSDFVKDYPRPIMPNMVFVGGINCLHQNPLSQEFEAYINASGEHGIVVFSLGSMVSEIPEKKAMAIADALGKIPQTVLWRYTGTRPSNLANNTILVKWLPQNDLLGHPMTRAFITHAGSHGVYESICNGVPMVMMPLFGDQMDNAKRMETKGAGVTLNVLEMTSEDLENALKAVINDKSYKENIMRLSSLHKDRPVEPLDLAVFWVEFVMRHKGAPHLRPAAHDLTWYQYHSLDVIGFLLAVVLTVAFITFKCCAYGYRKCLGKKGRVKKAHKSKTH
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Transferase
Function
UDP-glucuronosyltransferase (UGT) that catalyzes phase II biotransformation reactions in which lipophilic substrates are conjugated with glucuronic acid to increase the metabolite's water solubility, thereby facilitating excretion into either the urine or bile (PubMed:12181437, PubMed:15472229, PubMed:18004206, PubMed:18004212, PubMed:18719240, PubMed:19830808, PubMed:23288867). Essential for the elimination and detoxification of drugs, xenobiotics and endogenous compounds (PubMed:12181437, PubMed:18004206, PubMed:18004212). Catalyzes the glucuronidation of endogenous estrogen hormones such as estradiol, estrone and estriol (PubMed:15472229, PubMed:18719240, PubMed:23288867). Involved in the glucuronidation of bilirubin, a degradation product occurring in the normal catabolic pathway that breaks down heme in vertebrates (PubMed:17187418, PubMed:18004206, PubMed:19830808). Also catalyzes the glucuronidation the isoflavones genistein, daidzein, glycitein, formononetin, biochanin A and prunetin, which are phytoestrogens with anticancer and cardiovascular properties (PubMed:18052087, PubMed:19545173). Involved in the glucuronidation of the AGTR1 angiotensin receptor antagonist losartan, a drug which can inhibit the effect of angiotensin II (PubMed:18674515). Involved in the biotransformation of 7-ethyl-10-hydroxycamptothecin (SN-38), the pharmacologically active metabolite of the anticancer drug irinotecan (PubMed:12181437, PubMed:18004212, PubMed:20610558).
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Uniprot ID
Primary ID:
P22309

Secondarily ID:
A6NJC3
B8K286
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HGNC ID
HGNC:12530
Subcellular Location
Endoplasmic reticulum membrane
Cytoplasm
Perinuclear region
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000006 , HEK293
Compound ID Compound Name Compound Formula
CP0036175
1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[(2S)-3-methyl-2-{[methyl({[2-(propan-2-yl)-1,3-thiazol-4-yl]methyl})carbamoyl]amino}butanamido]-1,6-diphenylhexan-2-yl]carbamate
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C37H48N6O5S2
 2
1
IC50 = 1700 nM
   TI
   LI
   LO
   TS
2
IC50 = 3000 nM
   TI
   LI
   LO
   TS
CP0038975
2,6-Dihydroxyanthraquinone
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C14H8O4
 2
1
IC50 = 3600 nM
   TI
   LI
   LO
   TS
2
IC50 = 4000 nM
   TI
   LI
   LO
   TS
CP0027482
5,6,7-Trihydroxyflavone
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C15H10O5
 2
1
IC50 = 4400 nM
   TI
   LI
   LO
   TS
2
IC50 = 7000 nM
   TI
   LI
   LO
   TS
CP0041554
Thyroxine
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C15H11I4NO4
 2
1
IC50 = 4900 nM
   TI
   LI
   LO
   TS
2
IC50 = 5600 nM
   TI
   LI
   LO
   TS
CP0040158
7,4&#8242;-Dihydroxy-isoflavone (3a)
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C15H10O4
 1
1
IC50 = 7300 nM
   TI
   LI
   LO
   TS
CP0041757
1-(9H-carbazol-4-yloxy)-3-[2-(2-methoxyphenoxy)ethylamino]propan-2-ol
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C24H26N2O4
 2
1
IC50 = 12000 nM
   TI
   LI
   LO
   TS
2
IC50 = 27000 nM
   TI
   LI
   LO
   TS
CP0005212
US8987315, Ketoconazole
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C26H28Cl2N4O4
 2
1
IC50 = 13000 nM
   TI
   LI
   LO
   TS
2
IC50 = 27000 nM
   TI
   LI
   LO
   TS
CP0084320
CAS_4394-00-7
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C13H9F3N2O2
 2
1
IC50 = 13000 nM
   TI
   LI
   LO
   TS
2
IC50 = 53000 nM
   TI
   LI
   LO
   TS
CP0045125
17-ethinyl-3,17-estradiol
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C20H24O2
 2
1
IC50 = 21000 nM
   TI
   LI
   LO
   TS
2
IC50 = 44000 nM
   TI
   LI
   LO
   TS
CP0056340
(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-ol
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C15H26O
 2
1
IC50 = 40000 nM
   TI
   LI
   LO
   TS
2
IC50 = 47000 nM
   TI
   LI
   LO
   TS
CP0034803
4-Methyl-7-hydroxycoumarin
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C10H8O3
 1
1
IC50 = 100000 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0037356
7-ETHYL-10-HYDROXY-CAMPTOTHECIN
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C22H20N2O5
 2
1 Km = 24000 nM
2 Km = 25000 nM
Clinical Information about the Protein
Target 1 ( UDP-glucuronosyltransferase 1A1 (UGT1A1) )
Target Type Clinical trial Target