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Atlas / Gene / UGT2B7

UGT2B7

gene
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Also known as UGT2B9

Summary

UGT2B7 (UDP glucuronosyltransferase family 2 member B7, HGNC:12554) is a protein-coding gene on chromosome 4q13.2, encoding UDP-glucuronosyltransferase 2B7 (P16662). 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.

The protein encoded by this gene belongs to the UDP-glycosyltransferase (UGT) family. UGTs serve a major role in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. This protein is localized in the microsome membrane, and has unique specificity for 3,4-catechol estrogens and estriol, suggesting that it may play an important role in regulating the level and activity of these potent estrogen metabolites. Alternative splicing results in multiple transcript variants.

Source: NCBI Gene 7364 — RefSeq curated summary.

At a glance

  • GWAS associations: 9
  • Clinical variants (ClinVar): 188 total
  • Druggable target: yes — 1 molecules with ChEMBL bioactivity
  • MANE Select transcript: NM_001074

Identifiers

Gene identifiers

FieldValue
HGNC IDHGNC:12554
Approved symbolUGT2B7
NameUDP glucuronosyltransferase family 2 member B7
Location4q13.2
Locus typegene with protein product
StatusApproved
AliasesUGT2B9
Ensembl geneENSG00000171234
Ensembl biotypeprotein_coding
OMIM600068
Entrez7364

Gene structure

Transcript identifiers

Ensembl transcripts: 10 — 9 protein_coding, 1 protein_coding_CDS_not_defined

ENST00000305231, ENST00000502942, ENST00000508661, ENST00000509763, ENST00000622664, ENST00000868341, ENST00000868342, ENST00000868343, ENST00000868344, ENST00000868345

RefSeq mRNA: 3 — MANE Select: NM_001074 NM_001074, NM_001330719, NM_001349568

CCDS: CCDS3526, CCDS82930

Canonical transcript exons

ENST00000305231 — 6 exons

ExonStartEnd
ENSE000014048136911245769112987
ENSE000017792776909647469097241
ENSE000024630456910810369108322
ENSE000035100306910280769102938
ENSE000035491866909854069098688
ENSE000035710256910717569107262

Expression profiles

Bgee: expression breadth broad, 84 present calls, max score 98.38.

FANTOM5 (CAGE): breadth tissue_specific, TPM avg 1.2572 / max 363.7827, expressed in 96 samples.

FANTOM5 promoters (6 alternative TSS)

Promoter IDTPM avgSamples expressed
478360.979534
478330.104343
478370.075316
478310.054128
478380.02666
2031880.01746

Top tissues by expression

133 total, by Bgee expression score (0-100, higher = more expressed):

TissueAnatomy IDExpression scoreQuality
liverUBERON:000210798.38gold quality
right lobe of liverUBERON:000111498.18gold quality
adult mammalian kidneyUBERON:000008298.16gold quality
duodenumUBERON:000211496.36gold quality
kidneyUBERON:000211395.36gold quality
metanephros cortexUBERON:001053395.12gold quality
metanephric glomerulusUBERON:000473694.76gold quality
right uterine tubeUBERON:000130291.45gold quality
cortex of kidneyUBERON:000122588.58gold quality
endometriumUBERON:000129587.12gold quality
male germ line stem cell (sensu Vertebrata) in testisCL:0000089 ∩ UBERON:000047385.20gold quality
gall bladderUBERON:000211081.56gold quality
fallopian tubeUBERON:000388979.92gold quality
body of pancreasUBERON:000115079.35gold quality
pancreasUBERON:000126477.95gold quality
islet of LangerhansUBERON:000000677.12gold quality
rectumUBERON:000105276.97gold quality
small intestineUBERON:000210872.64gold quality
small intestine Peyer’s patchUBERON:000345471.44gold quality
mucosa of transverse colonUBERON:000499170.22gold quality
epithelium of bronchusUBERON:000203167.77gold quality
olfactory segment of nasal mucosaUBERON:000538667.08gold quality
minor salivary glandUBERON:000183064.45gold quality
saliva-secreting glandUBERON:000104463.77gold quality
left uterine tubeUBERON:000130362.61gold quality
vastus lateralisUBERON:000137960.65gold quality
quadriceps femorisUBERON:000137760.39gold quality
tracheaUBERON:000312659.07gold quality
dorsal plus ventral thalamusUBERON:000189759.03gold quality
dorsal root ganglionUBERON:000004458.67gold quality

Single-cell (SCXA)

Detected in 6 experiment(s), a significant marker in 6.

ExperimentMarker?Max mean expression
E-GEOD-131882yes817.32
E-GEOD-124472yes262.03
E-MTAB-10287yes46.56
E-CURD-119yes19.42
E-MTAB-6678yes8.59
E-ANND-3no0.00

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): CDX2, CEBPA, HNF1A, HNF4A, NFE2L2, NR1H4, NR1I2, NR1I3, POU2F1, TP53

miRNA regulators (miRDB)

9 targeting UGT2B7, top 30 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific):

miRNAMax scoreAvg scoremiRNA target_count
HSA-MIR-3064-3P100.0070.091254
HSA-MIR-397399.2069.191990
HSA-MIR-146A-3P99.1368.991881
HSA-MIR-6776-5P98.5467.431304
HSA-MIR-431798.4967.09987
HSA-MIR-448398.0964.121642
HSA-MIR-3664-3P97.8567.621452
HSA-MIR-7112-3P97.6768.77948
HSA-MIR-129396.1664.69916

Literature-anchored findings (GeneRIF, showing 40)

  • These results demonstrate for the first time glucuronidation of catechols by gastric and intestinal microsomal UGTs and three human recombinant UGT isoforms.Recombinant human UGT1A6, 1A9, and 2B7 effectively catalyzed catechol glucuronidation (PMID:12623074)
  • two human allelic variants UGT2B7H((268)) and UGT2B7Y((268)) conjugate aldosterone, its A-ring reduced metabolites (5alpha-dihydroaldosterone and 3alpha,5beta-tetrahydroaldosterone), and both 5alpha- and 5beta-tetrahydrocortisone epimers. (PMID:12746330)
  • interindividual differences in morphine glucuronidation may be the result of genetic variation in UGT2B7 (PMID:12811366)
  • a significant role for UGT1A9 and 2B7 in the catalysis of almokalant glucuronidation (PMID:14660172)
  • P. 1053 “…UGT2B7…is…fairly common in Caucasians…and Africans”…“but…still rare in Japanese…” P. 1054: “…genotyping…UGT2B7 in Japanese…would be useful for studies on…association between haplotypes and pharmacokinetic…paramters.” (PMID:15319348)
  • in liver microsomes, UGT1A1 is primarily responsible for farnesol glucuronidation; however, in intestine microsomes, UGT2B7 is probably the major isoform involved (PMID:15320866)
  • UGT2B7 demonstrated the highest catalytic activities for estrogens and at least 10- to 50-fold higher activity for the conjugation of genotoxic 4-hydroxycatecholestrogens at position 4 (PMID:15472229)
  • Cytochrome 450 3A4 alters UDPG glucuroyosyltransgferase regioselectivity so that the ratio of morphine activation/detoxication is increased. (PMID:15611481)
  • These results suggest that the haplotype structure of UGT2B7 in the Japanese population is different from that of other ethnic groups. (PMID:16466707)
  • Allelic variants of UGT2B7, CYP2C8, and ABCC2, which may predispose to the formation and accumulation of reactive diclofenac metabolites are associated with diclofenac hepatotoxicity (PMID:17241877)
  • Results strongly indicated that the presence of an aromatic residue at position 33 is important for the activity and specificity of UGT2B7. (PMID:17263731)
  • Provide evidence for HNF1alpha as a determinant of UGT2B7 mRNA expression, but suggest a role for multiple transcription factors. (PMID:17440429)
  • Results describe the crystal structure of the cofactor-binding domain of the human phase II drug-metabolism enzyme UDP-glucuronosyltransferase 2B7.( (PMID:17442341)
  • Formation of (R)- and (S)-glucuronide from racemic flurbiprofen is catalyzed by UGT2B7. (PMID:17446261)
  • The UGT2B7 H(268)Y polymorphism is independently associated with cortical bone size and serum sex steroid levels in young adult men. (PMID:17579197)
  • Results suggest that UGT2B7 is the main isozyme responsible for gemfibrozil glucuronidation in humans. (PMID:17670842)
  • The UGT2B7 genotype probably affects lorazepam-valproate pharmacodynamic interaction, especially in subjects who have homovariant genotypes of UGT2B7 and UGT2B15, although the effects on the pharmacokinetics are less significant. (PMID:17687269)
  • analysis of the human UDP-glucuronosyltransferase 2B7 and its inhibitors (PMID:17706742)
  • Presence of UGT2B7 -840G allele is associated with significantly reduced glucuronidation of morphine and thus contributes to the variability in hepatic clearance of morphine in sickle cell anemia. (PMID:17724700)
  • UGT2B7*3 allele did not significantly affect the systemic clearance/bioavailability of carvedilol enantiomers. (PMID:17965522)
  • UGT2B7 prefers metabolizing S-carvedilol to R-carvedilol. Both A71S and H268Y mutations of UGT2B7 reduced capacity but did not affect affinity and, as a result, the efficiency of metabolism was remarkably reduced. (PMID:17978490)
  • There was no relevant association between the identified UGT2B7 genotypes and increased bladder cancer occurrence in the two investigated Caucasian groups in Germany. (PMID:18569595)
  • Haplotype 4 was associated with an increase in enzyme activity and gene expression. (PMID:18622261)
  • UGT2B7 is transcriptionally regulated by Nrf2, but the mechanism is hindered by polymorphisms in the promoter region of UGT2B7*2. (PMID:18622263)
  • Kinetic modeling of the interactions between 4-methylumbelliferone, 1-naphthol, and zidovudine glucuronidation by UGT2B7 provides evidence for multiple substrate binding and effector sites. (PMID:18647858)
  • the effect of UGT2B7 polymorphism on the pharmacokinetics of mycophenolic acid (MPA) and its metabolites phenolic glucuronide (MPAG) and acyl glucuronide (AcMPAG) in Chinese renal transplant (PMID:18946804)
  • Our results strongly suggested that UGT2B7 is not expressed in normal breast tissue. (PMID:19116784)
  • These data are consistent with Src-based 2B7 glucuronidation of genotoxic catechol estrogens in mammary gland. (PMID:19289110)
  • Genetic variations in UGT2B7 and endometrial cancer risk (PMID:19352303)
  • Genetic polymorphism in UDP-glucuronosyltransferase 2B7 is associated with colorectal cancer. (PMID:19408577)
  • analysis of stereoselective metabolism of propranolol glucuronidation by human UDP-glucuronosyltransferases 2B7 and 1A9 (PMID:19644937)
  • findings demonstrate independent effects of CYP2A6 and UGT2B7 genetic variation on efavirenz disposition beyond that of the CYP2B6 polymorphisms. (PMID:19779319)
  • results suggest that UGT2B7 is the primary human hepatic UDP-glucuronosyltransferase isoform catalyzing 3-O- and 1-O-CP glucuronidation with minor contributions from UGT1A6 and UGT1A9 (PMID:20008037)
  • UGT2B7_-161C>T polymorphism is significantly associated with lamotrigine concentration-to-dose ratio. (PMID:20216122)
  • The results also indicated that UGT1A1, UGT1A7, UGT1A8, UGT1A9, UGT1A10 and UGT2B7 are the most important six UGT isoforms for metabolizing the three dihydroxyflavones and seven monohydroxyflavones. (PMID:20297805)
  • UGT2B7 and UGT1A7 heterozygosity predicted increased apparent oral clearance of mycophenolic acid (MPA). (PMID:20567810)
  • Identification of UGT2B7 single nucleotide polymorphisms with LD and the tagging SNPs lays the foundation for investigating UGT2B7-related genotype/phenotype association studies for Koreans as well as other populations. (PMID:20814162)
  • 2B7 substrate selection is not fixed but varies depending upon the tyrosine kinases that carry out its required phosphorylation (PMID:21056984)
  • Diabetes mellitus is associated with significantly reduced UGT2B7 mRNA expression, protein level, and enzymatic activity of liver and kidney. (PMID:21123165)
  • results suggest that HNF4alpha plays an important role in the constitutive expression of hepatic UGT2B7, and CAR acts as a negative regulator by interfering with HNF4alpha binding activity (PMID:21415305)

Cross-species orthologs

107 orthologs

OrganismSymbolGene ID
danio_reriougt5d1ENSDARG00000002394
danio_reriougt5c2ENSDARG00000006372
danio_reriougt5a1ENSDARG00000016479
danio_reriougt5g1ENSDARG00000032862
danio_reriougt5g2ENSDARG00000043901
danio_reriougt5f1ENSDARG00000054835
danio_reriougt5e1ENSDARG00000058048
danio_reriougt5c3ENSDARG00000061439
danio_reriougt5c1ENSDARG00000061444
danio_reriosi:ch73-334d15.1ENSDARG00000061672
danio_reriougt2a7ENSDARG00000091624
danio_reriougt5b4ENSDARG00000091916
danio_reriougt2b1ENSDARG00000093043
danio_reriougt5a2ENSDARG00000093640
danio_reriougt5b3ENSDARG00000099276
danio_reriougt5b2ENSDARG00000101495
danio_reriougt5b5ENSDARG00000104203
danio_reriougt5b1ENSDARG00000104995
danio_reriougt2b3ENSDARG00000109611
danio_rerioENSDARG00000110614
danio_rerioENSDARG00000113218
danio_reriougt2b5ENSDARG00000116986
drosophila_melanogasterUgt36A1FBGN0015663
drosophila_melanogasterUgt35B1FBGN0026314
drosophila_melanogasterUgt35A1FBGN0026315
drosophila_melanogasterUgt37C1FBGN0026754
drosophila_melanogasterUgt37B1FBGN0026755
drosophila_melanogasterUgt37A1FBGN0026756
drosophila_melanogasterUgt36E1FBGN0027070
drosophila_melanogasterUgt49B1FBGN0027073
drosophila_melanogasterUgt36F1FBGN0027074
drosophila_melanogasterUgt307A1FBGN0031887
drosophila_melanogasterUgt36D1FBGN0032713
drosophila_melanogasterUgt49C1FBGN0034605
drosophila_melanogasterUgt316A1FBGN0036842
drosophila_melanogasterUgt37A2FBGN0038082
drosophila_melanogasterUgt37A3FBGN0038083
drosophila_melanogasterUgt49B2FBGN0038886
drosophila_melanogasterUgt303B3FBGN0039085
drosophila_melanogasterUgt303B1FBGN0039086
drosophila_melanogasterUgt303B2FBGN0039087
drosophila_melanogasterUgt304A1FBGN0040250
drosophila_melanogasterUgt302K1FBGN0040251
drosophila_melanogasterUgt303A1FBGN0040252
drosophila_melanogasterUgt35E1FBGN0040253
drosophila_melanogasterUgt35E2FBGN0040255
drosophila_melanogasterUgt302E1FBGN0040257
drosophila_melanogasterUgt302C1FBGN0040259
drosophila_melanogasterUgt37D1FBGN0040260
drosophila_melanogasterUgt37E1FBGN0040261
drosophila_melanogasterUgt37C2FBGN0040262
drosophila_melanogasterUgt305A1FBGN0042179
drosophila_melanogasterUgt35D1FBGN0051002
caenorhabditis_elegansWBGENE00007072
caenorhabditis_elegansWBGENE00007073
caenorhabditis_elegansWBGENE00007402
caenorhabditis_elegansWBGENE00007422
caenorhabditis_elegansWBGENE00007455
caenorhabditis_elegansWBGENE00007885
caenorhabditis_elegansWBGENE00007946
caenorhabditis_elegansWBGENE00008097
caenorhabditis_elegansWBGENE00008486
caenorhabditis_elegansWBGENE00009255
caenorhabditis_elegansWBGENE00010904
caenorhabditis_elegansWBGENE00011006
caenorhabditis_elegansWBGENE00011340
caenorhabditis_elegansWBGENE00011452
caenorhabditis_elegansWBGENE00011453
caenorhabditis_elegansWBGENE00012788
caenorhabditis_elegansWBGENE00013900
caenorhabditis_elegansWBGENE00013905
caenorhabditis_elegansWBGENE00013906
caenorhabditis_elegansWBGENE00015141
caenorhabditis_elegansWBGENE00015369
caenorhabditis_elegansWBGENE00015371
caenorhabditis_elegansWBGENE00015449
caenorhabditis_elegansWBGENE00015577
caenorhabditis_elegansugt-28WBGENE00015693
caenorhabditis_elegansugt-27WBGENE00015694
caenorhabditis_elegansugt-26WBGENE00015695
caenorhabditis_elegansWBGENE00015739
caenorhabditis_elegansWBGENE00015965
caenorhabditis_elegansWBGENE00016013
caenorhabditis_elegansWBGENE00017315
caenorhabditis_elegansWBGENE00017329
caenorhabditis_elegansWBGENE00017331
caenorhabditis_elegansWBGENE00017332
caenorhabditis_elegansWBGENE00017333
caenorhabditis_elegansWBGENE00017334
caenorhabditis_elegansWBGENE00017336
caenorhabditis_elegansWBGENE00017959
caenorhabditis_elegansWBGENE00018206
caenorhabditis_elegansWBGENE00018543
caenorhabditis_elegansWBGENE00018931
caenorhabditis_elegansWBGENE00019232
caenorhabditis_elegansWBGENE00019233
caenorhabditis_elegansWBGENE00019234
caenorhabditis_elegansWBGENE00019235
caenorhabditis_elegansWBGENE00019515
caenorhabditis_elegansWBGENE00019516
caenorhabditis_elegansWBGENE00020587
caenorhabditis_elegansWBGENE00020592
caenorhabditis_elegansWBGENE00020593
caenorhabditis_elegansWBGENE00020594
caenorhabditis_elegansWBGENE00021709
caenorhabditis_elegansWBGENE00044282
caenorhabditis_elegansWBGENE00044286

Paralogs (21): UGT2B10 (ENSG00000109181), UGT2A3 (ENSG00000135220), UGT2B28 (ENSG00000135226), UGT3A1 (ENSG00000145626), UGT2B4 (ENSG00000156096), UGT1A6 (ENSG00000167165), UGT3A2 (ENSG00000168671), UGT2A1 (ENSG00000173610), UGT8 (ENSG00000174607), UGT2B15 (ENSG00000196620), UGT2B17 (ENSG00000197888), UGT2B11 (ENSG00000213759), UGT1A9 (ENSG00000241119), UGT1A1 (ENSG00000241635), UGT1A8 (ENSG00000242366), UGT1A10 (ENSG00000242515), UGT1A7 (ENSG00000244122), UGT1A4 (ENSG00000244474), UGT2A2 (ENSG00000271271), UGT1A3 (ENSG00000288702), UGT1A5 (ENSG00000288705)

Protein

Protein identifiers

UDP-glucuronosyltransferase 2B7 — P16662 (reviewed: P16662)

Alternative names: 3,4-catechol estrogen-specific UDPGT, UDP-glucuronosyltransferase 2B9, UDPGTh-2

All UniProt accessions (4): A0A087X084, D6RH08, E9PBP8, P16662

UniProt curated annotations — full annotation on UniProt →

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. Essential for the elimination and detoxification of drugs, xenobiotics and endogenous compounds. Catalyzes the glucuronidation of endogenous steroid hormones such as androgens (epitestosterone, androsterone) and estrogens (estradiol, epiestradiol, estriol, catechol estrogens). Also regulates the levels of retinoic acid, a major metabolite of vitamin A involved in apoptosis, cellular growth and differentiation, and embryonic development. Contributes to bile acid (BA) detoxification by catalyzing the glucuronidation of BA substrates, which are natural detergents for dietary lipids absorption. Involved in the glucuronidation of arachidonic acid (AA) and AA-derived eicosanoids including 15-HETE, 20-HETE, PGE2, PGB1 and F2-isoprostanes (8-iso-PGF2alpha and 5-epi-5-F2t-IsoP). Involved in the glucuronidation of the phytochemical ferulic acid at the phenolic or the carboxylic acid group. Involved in the glucuronidation of the AGTR1 angiotensin receptor antagonist losartan, caderastan and zolarsatan, drugs which can inhibit the effect of angiotensin II. Also metabolizes mycophenolate, an immunosuppressive agent.

Subcellular location. Endoplasmic reticulum membrane.

Polymorphism. 2 alleles have been identified: UGT2B71 (His-268) and UGT2B72 (Tyr-268). The sequence shown is that of allele UGT2B7*2.

Similarity. Belongs to the UDP-glycosyltransferase family.

RefSeq proteins (3): NP_001065, NP_001317648, NP_001336497 (=MANE)

Domains & families (InterPro)

IDNameType
IPR002213UDP_glucos_transFamily
IPR035595UDP_glycos_trans_CSConserved_site
IPR050271UDP-glycosyltransferaseFamily

Pfam: PF00201

Enzyme classification (BRENDA):

  • EC 2.4.1.17 — glucuronosyltransferase (BRENDA: 32 organisms, 1285 substrates, 660 inhibitors, 855 Km, 6 kcat entries)

Substrate kinetics (BRENDA)

189 substrates with measured Km, best-characterized 15. Km ranges are aggregated across organisms/conditions.

SubstrateKm (mM)Measurements
4-METHYLUMBELLIFERONE0.0001–4.20444
MORPHINE0.0355–37.431
4-NITROPHENOL0.0102–224
PROPOFOL0.0072–0.919
ZIDOVUDINE0.508–1.5419
1-NAPHTHOL0.0025–2718
IMIPRAMINE0.0072–1.44213
TRANS-4-HYDROXYTAMOXIFEN0.0037–0.31913
SCOPOLETIN0.061–7.6411
SEROTONIN3.7–55.911
2-HYDROXYESTRONE0.0102–610
CIS-4-HYDROXYTAMOXIFEN0.0074–0.19310
DOPAMINE1.89–3.1110
1-HYDROXYBENZO(A)PYRENE0.0113–2.8699
1-HYDROXYPYRENE0.0032–2.3269

Catalyzed reactions (Rhea), 12 shown:

  • glucuronate acceptor + UDP-alpha-D-glucuronate = acceptor beta-D-glucuronoside + UDP + H(+) (RHEA:21032)
  • 16alpha-hydroxyestrone + UDP-alpha-D-glucuronate = 16alpha-hydroxyestrone 16-O-(beta-D-glucuronate) + UDP + H(+) (RHEA:52452)
  • 17beta-estradiol + UDP-alpha-D-glucuronate = 17beta-estradiol 17-O-(beta-D-glucuronate) + UDP + H(+) (RHEA:52464)
  • 16alpha,17beta-estriol + UDP-alpha-D-glucuronate = 16alpha,17beta-estriol 16-O-(beta-D-glucuronate) + UDP + H(+) (RHEA:52472)
  • epitestosterone + UDP-alpha-D-glucuronate = epitestosterone 17-O-(beta-D-glucuronate) + UDP + H(+) (RHEA:52568)
  • 17alpha-estradiol + UDP-alpha-D-glucuronate = 17alpha-estradiol 17-O-(beta-D-glucuronate) + UDP + H(+) (RHEA:52872)
  • 16beta,17beta-estriol + UDP-alpha-D-glucuronate = 16beta,17beta-estriol 16-O-(beta-D-glucuronate) + UDP + H(+) (RHEA:52880)
  • 16alpha,17alpha-estriol + UDP-alpha-D-glucuronate = 16alpha,17alpha-estriol 17-O-(beta-D-glucuronate) + UDP + H(+) (RHEA:52916)
  • 16alpha,17alpha-estriol + UDP-alpha-D-glucuronate = 16alpha,17alpha-estriol 16-O-(beta-D-glucuronate) + UDP + H(+) (RHEA:52920)
  • hyodeoxycholate + UDP-alpha-D-glucuronate = hyodeoxycholate 6-O-(beta-D-glucuronate) + UDP + H(+) (RHEA:52964)
  • hyocholate + UDP-alpha-D-glucuronate = hyocholate 6-O-(beta-D-glucuronate) + UDP + H(+) (RHEA:52968)
  • 2-hydroxy-17beta-estradiol + UDP-alpha-D-glucuronate = 2-hydroxy-17beta-estradiol 3-O-(beta-D-glucuronate) + UDP + H(+) (RHEA:53004)

UniProt features (39 total): mutagenesis site 11, helix 7, strand 6, turn 4, sequence variant 3, glycosylation site 3, binding site 2, signal peptide 1, chain 1, transmembrane region 1

Structure

Experimental structures (PDB)

1 structures.

PDBMethodResolution (Å)
2O6LX-RAY DIFFRACTION1.8

Predicted structure (AlphaFold)

ModelpLDDTFraction very-high
AF-P16662-F193.370.87

Functional residue map

Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.

Ligand- & substrate-binding residues (2): 373–379; 398

Glycosylation sites (3): 67, 68, 315

Mutagenesis-validated functional residues (11):

PositionPhenotype
15reduced androsterone, hyodeoxycholic acid and tetrachlorocatechol glucuronosyltransferase activities.
35reduced androsterone, hyodeoxycholic acid and tetrachlorocatechol glucuronosyltransferase activities.
151reduced androsterone and tetrachlorocatechol glucuronosyltransferase activities; abolished hyodeoxycholic acid glucurono
151abolished androsterone glucuronosyltransferase activity; reduced hyodeoxycholic acid and tetrachlorocatechol glucuronosy
373reduced androsterone, hyodeoxycholic acid and tetrachlorocatechol glucuronosyltransferase activities.
374abolished androsterone glucuronosyltransferase activity; reduced hyodeoxycholic acid and tetrachlorocatechol glucuronosy
378abolished androsterone glucuronosyltransferase activity; reduced hyodeoxycholic acid and tetrachlorocatechol glucuronosy
379abolished androsterone glucuronosyltransferase activity; reduced hyodeoxycholic acid and tetrachlorocatechol glucuronosy
379abolished androsterone glucuronosyltransferase activity; no change in hyodeoxycholic acid and tetrachlorocatechol glucur
398reduced androsterone, hyodeoxycholic acid and tetrachlorocatechol glucuronosyltransferase activities.
399abolished androsterone, hyodeoxycholic acid and tetrachlorocatechol glucuronosyltransferase activities.

Function

Pathways and Gene Ontology

Reactome pathways

3 pathways

IDPathway
R-HSA-156588Glucuronidation
R-HSA-9749641Aspirin ADME
R-HSA-9757110Prednisone ADME

MSigDB gene sets: 0 (showing top):

GO Biological Process (5): lipid metabolic process (GO:0006629), xenobiotic metabolic process (GO:0006805), androgen metabolic process (GO:0008209), estrogen metabolic process (GO:0008210), steroid metabolic process (GO:0008202)

GO Molecular Function (4): glucuronosyltransferase activity (GO:0015020), UDP-glycosyltransferase activity (GO:0008194), transferase activity (GO:0016740), glycosyltransferase activity (GO:0016757)

GO Cellular Component (3): endoplasmic reticulum membrane (GO:0005789), membrane (GO:0016020), endoplasmic reticulum (GO:0005783)

Reactome top-level categories

Rollup of top-2 pathways:

CategoryPathways
Drug ADME2
Phase II - Conjugation of compounds1

GO top-level categories

Rollup of top GO terms by namespace:

CategoryTerms
steroid metabolic process2
hormone metabolic process2
primary metabolic process1
metabolic process1
cellular response to xenobiotic stimulus1
lipid metabolic process1
UDP-glycosyltransferase activity1
hexosyltransferase activity1
glycosyltransferase activity1
catalytic activity1
transferase activity1
organelle membrane1
nuclear outer membrane-endoplasmic reticulum membrane network1
endoplasmic reticulum subcompartment1
cellular anatomical structure1
cytoplasm1
endomembrane system1
intracellular membrane-bounded organelle1

Protein interactions and networks

STRING

1026 interactions, top by confidence (×1000):

Protein AProtein BPartner UniProtScore
UGT2B7SLC35A2P78381967
UGT2B7CYP3A4P05184955
UGT2B7B3GAT2Q9NPZ5914
UGT2B7CYP2C8P10632817
UGT2B7PPIGQ13427790
UGT2B7CYP2C9P11712778
UGT2B7CYP2D6P10635777
UGT2B7CYP2C19P33259777
UGT2B7CYP2B6P20813775
UGT2B7ABCC2Q92887775
UGT2B7CYP1A2P05177734
UGT2B7CYP3A5P20815726
UGT2B7CYP2A6P00190718
UGT2B7HNF1AP20823717
UGT2B7SLCO1B1Q9Y6L6700

IntAct

10 interactions, top by confidence:

ABTypeScore
UGT1A9UGT2B7psi-mi:“MI:2364”(proximity)0.470
UGT2B7UGT1A1psi-mi:“MI:2364”(proximity)0.470
UGT2B7UGT1A1psi-mi:“MI:0915”(physical association)0.470
UGT1A9UGT2B7psi-mi:“MI:0915”(physical association)0.470
UGT2B7psi-mi:“MI:0559”(glycosylation reaction)0.440
UGT2B7GABRA3psi-mi:“MI:0915”(physical association)0.370
UGT2B7ACTN4psi-mi:“MI:0914”(association)0.350

BioGRID (7): CYP3A4 (Affinity Capture-Western), CYP3A4 (Far Western), UGT2B7 (Affinity Capture-Western), CYP3A4 (Affinity Capture-Western), UGT2B7 (Affinity Capture-Western), UGT2B7 (Affinity Capture-MS), UGT2B7 (Two-hybrid)

ESM2 similar proteins: A0A291PQF1, A0A291PQG3, A0A291PQH4, A8WLF6, O16881, O19103, O75310, P08541, P08542, P09875, P16662, P17717, P18569, P19488, P34317, P36511, P36513, P36537, Q09426, Q10941, Q10944, Q16880, Q18081, Q1LZI1, Q20086, Q21706, Q22180, Q22181, Q22295, Q25489, Q27757, Q3SY77, Q3UP75, Q5RFJ3, Q62789, Q63ZR6, Q64676, Q6K1J1, Q6NUS8, Q6PDD0

Diamond homologs: A0A0C1EH92, A0A0G2EAR7, A0A0M4KE44, A0A193AUF6, A0A1L7U2E9, A0A291PQF1, A0A291PQG3, A0A2R6Q8R5, A0A2R6QXF8, A0A2Z5CV93, A0A364KRL8, A0A478EC03, A0AAW1M2U7, A6XNC6, D3UAG0, F8WKW8, G2WW48, O02663, O23382, O31853, O60656, O75310, O81498, P08430, P0DO67, P0DO71, P0DO73, P0DTE4, P0DTE5, P14726, P16165, P16166, P16167, P16662, P20720, P22309, P22310, P35503, P35504, P36537

SIGNOR signaling

1 interactions.

AEffectBMechanism
SRCup-regulatesUGT2B7phosphorylation

Disease & clinical

Clinical variants and AI predictions

ClinVar

188 variants total. Per-class counts are floors (≥ shown; pagination cap):

ClassificationCount (floor)
Pathogenic0
Likely pathogenic0
Uncertain significance53
Likely benign3
Benign1

Top pathogenic / likely-pathogenic (0)

SpliceAI

1305 predictions. Top by Δscore:

VariantEffectΔscore
4:69098529:A:AGacceptor_gain1.0000
4:69098530:T:Gacceptor_gain1.0000
4:69098534:T:Aacceptor_gain1.0000
4:69098538:A:AGacceptor_gain1.0000
4:69098539:G:GGacceptor_gain1.0000
4:69098539:GGAA:Gacceptor_gain1.0000
4:69098686:AAGG:Adonor_loss1.0000
4:69098688:GGT:Gdonor_loss1.0000
4:69098689:G:GAdonor_loss1.0000
4:69098690:T:Gdonor_loss1.0000
4:69102802:CACA:Cacceptor_loss1.0000
4:69102805:A:Tacceptor_loss1.0000
4:69102806:GGAA:Gacceptor_gain1.0000
4:69102934:AAAAG:Adonor_loss1.0000
4:69102937:AGGTA:Adonor_loss1.0000
4:69102939:GTAAG:Gdonor_loss1.0000
4:69102940:T:Gdonor_loss1.0000
4:69107260:TAGGT:Tdonor_loss1.0000
4:69107261:AGG:Adonor_loss1.0000
4:69107262:GGTAA:Gdonor_loss1.0000
4:69107263:G:Cdonor_loss1.0000
4:69107263:G:GGdonor_gain1.0000
4:69108302:GAGA:Gdonor_gain1.0000
4:69108319:CTTC:Cdonor_gain1.0000
4:69108320:TTC:Tdonor_gain1.0000
4:69108323:G:GGdonor_gain1.0000
4:69112452:TTCA:Tacceptor_loss1.0000
4:69112453:TCA:Tacceptor_loss1.0000
4:69112455:A:AGacceptor_gain1.0000
4:69112455:A:Cacceptor_loss1.0000

AlphaMissense

3527 scored. Top likely-pathogenic:

VariantProtein changeam_pathogenicity
4:69107181:T:AW337R0.991
4:69107181:T:CW337R0.991
4:69108159:G:CA383P0.984
4:69107257:T:CL362P0.983
4:69107249:G:CQ359H0.979
4:69107249:G:TQ359H0.979
4:69096657:T:CL46P0.977
4:69108127:T:AI372K0.977
4:69096953:T:CF145L0.974
4:69096955:T:AF145L0.974
4:69096955:T:GF145L0.974
4:69102850:T:AV305E0.974
4:69097031:A:CS171R0.973
4:69097033:T:AS171R0.973
4:69097033:T:GS171R0.973
4:69108123:T:CF371L0.973
4:69108125:T:AF371L0.973
4:69108125:T:GF371L0.973
4:69102909:G:CA325P0.972
4:69108246:G:CA412P0.972
4:69107240:G:CW356C0.971
4:69107240:G:TW356C0.971
4:69108121:C:AA370D0.971
4:69112542:T:CF466L0.971
4:69112544:T:AF466L0.971
4:69112544:T:GF466L0.971
4:69107176:T:AV335D0.969
4:69107238:T:AW356R0.969
4:69107238:T:CW356R0.969
4:69097150:G:CR210S0.967

dbSNP variants (sampled 300 via entrez): RS1000002459 (4:69097347 G>A,T), RS1000012891 (4:69083969 A>G), RS1000033611 (4:69096990 G>A), RS1000102006 (4:69054128 A>G), RS1000109046 (4:69090984 C>A,T), RS1000136396 (4:69086309 T>C), RS1000144163 (4:69064619 C>A), RS1000153564 (4:69106623 G>A,T), RS1000184223 (4:69103406 A>G), RS1000246657 (4:69091314 C>T), RS1000352662 (4:69070232 A>G), RS1000395448 (4:69059283 C>T), RS1000454588 (4:69091864 T>C), RS1000480876 (4:69063354 A>G), RS1000492181 (4:69063037 A>G)

Disease associations

OMIM: gene MIM:600068 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

0 total (0 of 0 shown, HPO-id order):

GWAS associations

9 associations (top):

StudyTraitp-value
GCST001762_192Obesity-related traits2.000000e-07
GCST002883_1AR-C124910XX levels in individuals with acute coronary syndromes treated with ticagrelor8.000000e-14
GCST007684_1Plasma clozapine-norclozapine ratio in treatment-resistant schizophrenia9.000000e-66
GCST007684_3Plasma clozapine-norclozapine ratio in treatment-resistant schizophrenia4.000000e-13
GCST009144_26Disease progression in age-related macular degeneration (adjusted for baseline)3.000000e-06
GCST009733_9Urinary metabolite levels in chronic kidney disease2.000000e-14
GCST011349_49Gamma glutamyl transferase levels5.000000e-09
GCST90013406_180Liver enzyme levels (alkaline phosphatase)3.000000e-12
GCST90020091_3Estradiol levels4.000000e-18

EFO canonical traits (8, from GWAS)

EFO IDTrait name
EFO:0005112gestational age
EFO:0007020AR-C124910XX measurement
EFO:0600040plasma clozapine-to-N-desmethylclozapine ratio measurement
EFO:0008336disease progression measurement
EFO:0005116urinary metabolite measurement
EFO:0004532serum gamma-glutamyl transferase measurement
EFO:0004533alkaline phosphatase measurement
EFO:0004697estradiol measurement

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (2): CHEMBL4370 (SINGLE PROTEIN), CHEMBL4523985 (PROTEIN FAMILY)

Molecules with ChEMBL bioactivity

1 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 87,659 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

MoleculeNamePhasePatents
CHEMBL866MYCOPHENOLIC ACID487,659

PharmGKB: 1 entry (VIP=true, CPIC=false)

PharmGKB clinical annotations

36 annotations.

VariantTypeLevelDrugsPhenotypes
rs10028494Efficacy3fentanylPain;Postoperative
rs11940316Efficacy,Toxicity3methadoneOpioid-Related Disorders
rs12233719Metabolism/PK3valproic acidEpilepsy
rs28365062Other3zidovudine
rs28365062Metabolism/PK4efavirenzHIV infectious disease
rs28365063Metabolism/PK3carbamazepineEpilepsy
rs28365063Metabolism/PK4lamotrigineEpilepsy
rs4292394Efficacy,Toxicity3methadoneOpioid-Related Disorders
rs4554144Efficacy,Toxicity3methadoneOpioid-Related Disorders
rs4587017Efficacy3fentanylPain;Postoperative
rs61361928Metabolism/PK3ticagrelorAcute coronary syndrome
rs6600879Efficacy,Toxicity3methadoneOpioid-Related Disorders
rs6600880Efficacy,Toxicity3methadoneOpioid-Related Disorders
rs6600893Efficacy,Toxicity3methadoneOpioid-Related Disorders
rs7438135Toxicity3mycophenolate mofetilKidney Transplantation
rs7438135Efficacy,Toxicity3methadoneOpioid-Related Disorders
rs7438135Metabolism/PK3morphine
rs7439366Dosage3codeine
rs7439366Other4efavirenzHIV infectious disease
rs7439366Dosage4morphine
rs7439366Metabolism/PK4valproic acidEpilepsy
rs7439366Efficacy,Toxicity3methadoneOpioid-Related Disorders
rs7439366Efficacy3oxcarbazepineEpilepsy
rs7439366Efficacy3oxycodonePain
rs7439366Efficacy3morphinePain
rs7439366Metabolism/PK3morphine
rs7439366Efficacy3fentanylPain;Postoperative
rs7439366Metabolism/PK3buprenorphine / naloxoneOpioid-Related Disorders
rs7439366Metabolism/PK3levomethadone;methadone;S-EDDPOpioid-Related Disorders
rs7662029Efficacy,Toxicity3methadoneOpioid-Related Disorders
rs7662029Metabolism/PK3buprenorphine / naloxoneOpioid-Related Disorders
rs7668258Metabolism/PK3valproic acidEpilepsy
rs7668258Dosage3lamotrigineEpilepsy
rs7668258Efficacy3methadoneOpioid-Related Disorders
rs7668258Metabolism/PK3lamotrigineEpilepsy
rs7668282Metabolism/PK3morphineSickle Cell Anemia

PharmGKB variants

27 variants.

VariantGenesLevelScore#Clin annotsDrugs
rs4292394UGT2B733.251methadone
rs4554144UGT2B733.251methadone
rs6600879UGT2B733.251methadone
rs6600880UGT2B733.251methadone
rs6600893UGT2B733.501methadone
rs7438135UGT2B733.253morphine;mycophenolate mofetil;methadone
rs7438284UGT2B70.000
rs7439366UGT2B733.2512valproic acid;efavirenz;oxycodone;oxcarbazepine;codeine;buprenorphine / naloxone;methadone;fentanyl;levomethadone;methadone;S-EDDP;morphine
rs7662029UGT2B733.252methadone;buprenorphine / naloxone
rs7668258UGT2B733.254lamotrigine;valproic acid;methadone
rs7668282UGT2B731.001morphine
rs11940316UGT2B733.251methadone
rs12233719UGT2B731.501valproic acid
rs28365062UGT2B731.502zidovudine;efavirenz
rs28365063UGT2B731.502carbamazepine;lamotrigine
rs61361928UGT2B730.001ticagrelor
rs62298861UGT2B70.000
rs73823859UGT2B70.000
rs4455491UGT2B70.000
rs11931604UGT2B70.000
rs6851533UGT2B70.000
rs4587017UGT2B730.001fentanyl
rs10028494UGT2B732.251fentanyl
rs28375964UGT2B70.000
rs10006452UGT2B70.000
rs62296959UGT2B70.000
rs6827692UGT2B70.000

Binding affinities (BindingDB)

48 measured of 60 human assays (65 total across all organisms); most potent 48 below. Values come from heterogeneous assays and are not directly comparable.

LigandMeasureValuePatent
((1S,3aR,4S,8aR,9S)-4,8,8-trimethyl-decahydro-1,4-methano-azulen-9-yl)-methanolIC50100 nM
(1S)-2-chloro-1-[(1R,2S,7S,8S,9S)-3,3,7-trimethyltricyclo[5.4.0.02,9]undec-8-yl]ethanolIC50200 nM
(1R)-2-chloro-1-[(1R,2S,7S,8S,9S)-3,3,7-trimethyltricyclo[5.4.0.02,9]undec-8-yl]ethanolIC50200 nM
(1R)-1-[(1R,2S,7S,8S,9S)-3,3,7-trimethyltricyclo[5.4.0.02,9]undec-8-yl]propane-1,3-diolIC50200 nM
(1S)-1-[(1R,2S,7S,8S,9S)-3,3,7-trimethyltricyclo[5.4.0.02,9]undec-8-yl]but-3-en-1-olIC50200 nM
(1S)-2,2-dimethyl-1-[(1R,2S,7S,8S,9S)-3,3,7-trimethyltricyclo[5.4.0.02,9]undec-8-yl]propan-1-olIC50200 nM
4-Amino-N-(2-phenyl-2H-pyrazol-3-yl)-benzenesulfonamideIC50210 nMUS-9688624: DP2 antagonist and uses thereof
ethyl (3S)-3-hydroxy-3-[(1R,2S,7S,8S,9S)-3,3,7-trimethyltricyclo[5.4.0.02,9]undec-8-yl]propanoateIC50300 nM
(1S)-1-[(1R,2S,7S,8S,9S)-3,3,7-trimethyltricyclo[5.4.0.02,9]undec-8-yl]propane-1,3-diolIC50300 nM
(1R)-1-[(1R,2S,7S,8S,9S)-3,3,7-trimethyltricyclo[5.4.0.02,9]undec-8-yl]prop-2-en-1-olIC50300 nM
(1R)-2-methyl-1-[(1R,2S,7S,8S,9S)-3,3,7-trimethyltricyclo[5.4.0.02,9]undec-8-yl]propan-1-olIC50400 nM
(1S)-2-methyl-1-[(1R,2S,7S,8S,9S)-3,3,7-trimethyltricyclo[5.4.0.02,9]undec-8-yl]propan-1-olIC50400 nM
ethyl (3R)-3-hydroxy-3-[(1R,2S,7S,8S,9S)-3,3,7-trimethyltricyclo[5.4.0.02,9]undec-8-yl]propanoateIC50400 nM
(1R)-1-[(1R,2S,7S,8S,9S)-3,3,7-trimethyltricyclo[5.4.0.02,9]undec-8-yl]but-3-en-1-olIC50400 nM
2-[(1R,2S,7R,8S,9R)-3,3,7-trimethyltricyclo[5.4.0.02,9]undec-8-yl]ethanolIC50500 nM
(1S)-1-[(1R,2S,7S,8S,9S)-3,3,7-trimethyltricyclo[5.4.0.02,9]undec-8-yl]propan-1-olIC50500 nM
(1R)-1-[(1R,2S,7S,8S,9S)-3,3,7-trimethyltricyclo[5.4.0.02,9]undec-8-yl]propan-1-olIC50500 nM
(1R)-1-[(1R,2S,7S,8S,9S)-3,3,7-trimethyltricyclo[5.4.0.02,9]undec-8-yl]ethanolIC50500 nM
(1S)-1-[(1R,2S,7S,8S,9S)-3,3,7-trimethyltricyclo[5.4.0.02,9]undec-8-yl]prop-2-en-1-olIC50600 nM
(2Z)-3-[(1R,2S,7S,8S,9S)-3,3,7-trimethyltricyclo[5.4.0.02,9]undec-8-yl]prop-2-en-1-olIC50700 nM
(1S)-1-[(1R,2S,7S,8S,9S)-3,3,7-trimethyltricyclo[5.4.0.02,9]undec-8-yl]ethanolIC50700 nM
(1R)-2,2-dimethyl-1-[(1R,2S,7S,8S,9S)-3,3,7-trimethyltricyclo[5.4.0.02,9]undec-8-yl]propan-1-olIC50800 nM
(2E)-3-[(1R,2S,7S,8S,9S)-3,3,7-trimethyltricyclo[5.4.0.02,9]undec-8-yl]prop-2-en-1-olIC50800 nM
(3R)-3-hydroxy-3-[(1R,2S,7S,8S,9S)-3,3,7-trimethyltricyclo[5.4.0.02,9]undec-8-yl]propionic acidIC50900 nM
3-[(1R,2S,7R,8S,9R)-3,3,7-trimethyltricyclo[5.4.0.02,9]undec-8-yl]propan-1-olIC50900 nM
(1S)-phenyl-[(1R,2S,7S,8S,9S)-3,3,7-trimethyltricyclo[5.4.0.02,9]undec-8-yl]methanolIC50900 nM
(3S)-3-hydroxy-3-[(1R,2S,7S,8S,9S)-3,3,7-trimethyltricyclo[5.4.0.02,9]undec-8-yl]propionic acidIC501000 nM
(1S,3aR,4S,8aS,9S)-4,8,8-trimethyl-decahydro-1,4-methano-azulene-9-carboxylic acidIC502000 nM
3-[(1R,2S,7R,8S,9R)-3,3,7-trimethyltricyclo[5.4.0.02,9]undec-8-yl]propanoic acidIC502000 nM
3-(furan-2-ylmethyl)-1,8-dimethyl-1H-purine-2,6(3H,7H)-dioneIC502200 nMUS-9688624: DP2 antagonist and uses thereof
2-[(1R,2S,7R,8S,9R)-3,3,7-trimethyltricyclo[5.4.0.02,9]undec-8-yl]butan-1-olIC503000 nM
dimethyl {(3R)-3-hydroxy-3-[(1R,2S,7S,8S,9S)-3,3,7-trimethyltricyclo[5.4.0.02,9]undec-8-yl]propyl}phosphonateIC503000 nM
(2E)-3-[(1R,2S,7S,8S,9S)-3,3,7-trimethyltricyclo[5.4.0.02,9]undec-8-yl]acrylic acidIC503000 nM
(2Z)-3-[(1R,2S,7S,8S,9S)-3,3,7-trimethyltricyclo[5.4.0.02,9]undec-8-yl]acrylic acidIC503000 nM
dimethyl {(3S)-3-hydroxy-3-[(1R,2S,7S,8S,9S)-3,3,7-trimethyltricyclo[5.4.0.02,9]undec-8-yl]propyl}phosphonateIC504000 nM
diethyl {(3S)-3-hydroxy-3-[(1R,2S,7S,8S,9S)-3,3,7-trimethyltricyclo[5.4.0.02,9]undec-8-yl]propyl}phosphonateIC504000 nM
diethyl {(3R)-3-hydroxy-3-[(1R,2S,7S,8S,9S)-3,3,7-trimethyltricyclo[5.4.0.02,9]undec-8-yl]propyl}phosphonateIC505000 nM
CHEMBL1203943IC505000 nM
{(E)-2-[(1R,2S,7S,8R,9S)-3,3,7-trimethyltricyclo[5.4.0.02,9]undec-8-yl]vinyl}phosphonic acidIC508000 nM
diethyl {(2S)-2-hydroxy-2-[(1R,2S,7S,8S,9S)-3,3,7-trimethyltricyclo[5.4.0.02,9]undec-8-yl]ethyl}phosphonateIC5010000 nM
diethyl {(2R)-2-hydroxy-2-[(1R,2S,7S,8S,9S)-3,3,7-trimethyltricyclo[5.4.0.02,9]undec-8-yl]ethyl}phosphonateIC5010000 nM
{2-[(1R,2S,7R,8S,9R)-3,3,7-trimethyltricyclo[5.4.0.02,9]undec-8-yl]ethyl}phosphonic acidIC5012000 nM
4-[(1R,2S,7R,8S,9R)-3,3,7-trimethyltricyclo[5.4.0.02,9]undec-8-yl]butanoic acidIC5016000 nM
{(2S)-2-hydroxy-2-[(1R,2S,7S,8S,9S)-3,3,7-trimethyltricyclo[5.4.0.02,9]undec-8-yl]ethyl}phosphonic acidIC5018000 nM
{(3S)-3-hydroxy-3-[(1R,2S,7S,8S,9S)-3,3,7-trimethyltricyclo[5.4.0.02,9]undec-8-yl]propyl}phosphonic acidIC5018000 nM
{(3R)-3-hydroxy-3-[(1R,2S,7S,8S,9S)-3,3,7-trimethyltricyclo[5.4.0.02,9]undec-8-yl]propyl}phosphonic acidIC5028000 nM
{3-[(1R,2S,7R,8S,9R)-3,3,7-trimethyltricyclo[5.4.0.02,9]undec-8-yl]propyl}phosphonic acidIC5032000 nM
{(1E)-3-[(1R,2S,7R,8S,9R)-3,3,7-trimethyltricyclo[5.4.0.02,9]undec-8-yl]prop-1-en-1-yl}phosphonic acidIC5041000 nM

ChEMBL bioactivities

51 potent at pChembl≥5 of 60 total, top 45 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChemblTypeValueUnitMolecule
7.74Ki18.4nMCHEMBL376840
7.35Ki45nMCELASTROL
7.33IC5047nMCHEMBL376840
7.27IC5054nMCHEMBL376840
7.00IC50100nMISOLONGIFOLOL
6.70IC50200nMCHEMBL376839
6.70IC50200nMCHEMBL374179
6.70IC50200nMCHEMBL226038
6.70IC50200nMCHEMBL388191
6.70IC50200nMCHEMBL226514
6.52IC50300nMCHEMBL226088
6.52IC50300nMCHEMBL389041
6.52IC50300nMCHEMBL226344
6.40IC50400nMCHEMBL225769
6.40IC50400nMCHEMBL225768
6.40IC50400nMCHEMBL225767
6.40IC50400nMCHEMBL390574
6.30IC50500nMCHEMBL225520
6.30IC50500nMCHEMBL389256
6.30IC50500nMCHEMBL449400
6.30IC50500nMCHEMBL226039
6.22IC50600nMCHEMBL374178
6.16IC50700nMCHEMBL390748
6.16IC50700nMCHEMBL389042
6.10IC50800nMCHEMBL225521
6.10IC50800nMCHEMBL2448549
6.05IC50900nMCHEMBL390747
6.05IC50900nMCHEMBL225822
6.05IC50900nMCHEMBL226343
6.00IC501000nMCHEMBL390573
5.82Ki1500nMMYCOPHENOLIC ACID
5.70Ki2000nMMYCOPHENOLIC ACID
5.70IC502000nMCHEMBL439010
5.70IC502000nMISOLONGIFOLIC ACID
5.52IC503000nMCHEMBL387764
5.52IC503000nMCHEMBL226225
5.52IC503000nMCHEMBL225576
5.52IC503000nMCHEMBL387981
5.40IC504000nMCHEMBL226513
5.40IC504000nMCHEMBL226459
5.30IC505000nMCHEMBL1203943
5.30IC505000nMCHEMBL226460
5.10IC508000nMCHEMBL387765
5.00IC501e+04nMCHEMBL375253
5.00IC501e+04nMCHEMBL375252

PubChem BioAssay actives

51 with measured affinity, of 866 total; 42 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.

CompoundAssayTypeValueUnit
(R)-phenyl-[(1R,2S,7S,8S,9S)-3,3,7-trimethyl-8-tricyclo[5.4.0.02,9]undecanyl]methanol288412: Inhibition of human UGT2B7 assessed as reduction of estriol glucuronidationki0.0184uM
(2R,4aS,6aR,6aS,14aS,14bR)-10-hydroxy-2,4a,6a,6a,9,14a-hexamethyl-11-oxo-1,3,4,5,6,13,14,14b-octahydropicene-2-carboxylic acid1930630: Binding affinity to UGT2B7 (unknown origin) assessed as inhibition constantki0.0450uM
[(1R,2S,7S,8S,9S)-3,3,7-trimethyl-8-tricyclo[5.4.0.02,9]undecanyl]methanol288412: Inhibition of human UGT2B7 assessed as reduction of estriol glucuronidationic500.1000uM
(1S)-1-[(1R,2S,7S,8S,9S)-3,3,7-trimethyl-8-tricyclo[5.4.0.02,9]undecanyl]but-3-en-1-ol288412: Inhibition of human UGT2B7 assessed as reduction of estriol glucuronidationic500.2000uM
(1S)-2,2-dimethyl-1-[(1R,2S,7S,8S,9S)-3,3,7-trimethyl-8-tricyclo[5.4.0.02,9]undecanyl]propan-1-ol288412: Inhibition of human UGT2B7 assessed as reduction of estriol glucuronidationic500.2000uM
(1R)-1-[(1R,2S,7S,8S,9S)-3,3,7-trimethyl-8-tricyclo[5.4.0.02,9]undecanyl]propane-1,3-diol288412: Inhibition of human UGT2B7 assessed as reduction of estriol glucuronidationic500.2000uM
(1S)-2-chloro-1-[(1R,2S,7S,8S,9S)-3,3,7-trimethyl-8-tricyclo[5.4.0.02,9]undecanyl]ethanol288412: Inhibition of human UGT2B7 assessed as reduction of estriol glucuronidationic500.2000uM
(1R)-2-chloro-1-[(1R,2S,7S,8S,9S)-3,3,7-trimethyl-8-tricyclo[5.4.0.02,9]undecanyl]ethanol288412: Inhibition of human UGT2B7 assessed as reduction of estriol glucuronidationic500.2000uM
(1S)-1-[(1R,2S,7S,8S,9S)-3,3,7-trimethyl-8-tricyclo[5.4.0.02,9]undecanyl]propane-1,3-diol288412: Inhibition of human UGT2B7 assessed as reduction of estriol glucuronidationic500.3000uM
(1R)-1-[(1R,2S,7S,8S,9S)-3,3,7-trimethyl-8-tricyclo[5.4.0.02,9]undecanyl]prop-2-en-1-ol288412: Inhibition of human UGT2B7 assessed as reduction of estriol glucuronidationic500.3000uM
ethyl (3S)-3-hydroxy-3-[(1R,2S,7S,8S,9S)-3,3,7-trimethyl-8-tricyclo[5.4.0.02,9]undecanyl]propanoate288412: Inhibition of human UGT2B7 assessed as reduction of estriol glucuronidationic500.3000uM
(1R)-2-methyl-1-[(1R,2S,7S,8S,9S)-3,3,7-trimethyl-8-tricyclo[5.4.0.02,9]undecanyl]propan-1-ol288412: Inhibition of human UGT2B7 assessed as reduction of estriol glucuronidationic500.4000uM
ethyl (3R)-3-hydroxy-3-[(1R,2S,7S,8S,9S)-3,3,7-trimethyl-8-tricyclo[5.4.0.02,9]undecanyl]propanoate288412: Inhibition of human UGT2B7 assessed as reduction of estriol glucuronidationic500.4000uM
(1R)-1-[(1R,2S,7S,8S,9S)-3,3,7-trimethyl-8-tricyclo[5.4.0.02,9]undecanyl]but-3-en-1-ol288412: Inhibition of human UGT2B7 assessed as reduction of estriol glucuronidationic500.4000uM
(1S)-2-methyl-1-[(1R,2S,7S,8S,9S)-3,3,7-trimethyl-8-tricyclo[5.4.0.02,9]undecanyl]propan-1-ol288412: Inhibition of human UGT2B7 assessed as reduction of estriol glucuronidationic500.4000uM
(1S)-1-[(1R,2S,7S,8S,9S)-3,3,7-trimethyl-8-tricyclo[5.4.0.02,9]undecanyl]propan-1-ol288412: Inhibition of human UGT2B7 assessed as reduction of estriol glucuronidationic500.5000uM
2-[(1R,2S,7R,8S,9R)-3,3,7-trimethyl-8-tricyclo[5.4.0.02,9]undecanyl]ethanol288412: Inhibition of human UGT2B7 assessed as reduction of estriol glucuronidationic500.5000uM
(1R)-1-[(1R,2S,7S,8S,9S)-3,3,7-trimethyl-8-tricyclo[5.4.0.02,9]undecanyl]propan-1-ol288412: Inhibition of human UGT2B7 assessed as reduction of estriol glucuronidationic500.5000uM
(1R)-1-[(1R,2S,7S,8S,9S)-3,3,7-trimethyl-8-tricyclo[5.4.0.02,9]undecanyl]ethanol288412: Inhibition of human UGT2B7 assessed as reduction of estriol glucuronidationic500.5000uM
(1S)-1-[(1R,2S,7S,8S,9S)-3,3,7-trimethyl-8-tricyclo[5.4.0.02,9]undecanyl]prop-2-en-1-ol288412: Inhibition of human UGT2B7 assessed as reduction of estriol glucuronidationic500.6000uM
(Z)-3-[(1R,2S,7S,8S,9S)-3,3,7-trimethyl-8-tricyclo[5.4.0.02,9]undecanyl]prop-2-en-1-ol288412: Inhibition of human UGT2B7 assessed as reduction of estriol glucuronidationic500.7000uM
(1S)-1-[(1R,2S,7S,8S,9S)-3,3,7-trimethyl-8-tricyclo[5.4.0.02,9]undecanyl]ethanol288412: Inhibition of human UGT2B7 assessed as reduction of estriol glucuronidationic500.7000uM
(E)-3-[(1R,2S,7S,8S,9S)-3,3,7-trimethyl-8-tricyclo[5.4.0.02,9]undecanyl]prop-2-en-1-ol288412: Inhibition of human UGT2B7 assessed as reduction of estriol glucuronidationic500.8000uM
(1R)-2,2-dimethyl-1-[(1R,2S,7S,8S,9S)-3,3,7-trimethyl-8-tricyclo[5.4.0.02,9]undecanyl]propan-1-ol288412: Inhibition of human UGT2B7 assessed as reduction of estriol glucuronidationic500.8000uM
(S)-phenyl-[(1R,2S,7S,8S,9S)-3,3,7-trimethyl-8-tricyclo[5.4.0.02,9]undecanyl]methanol288412: Inhibition of human UGT2B7 assessed as reduction of estriol glucuronidationic500.9000uM
(3R)-3-hydroxy-3-[(1R,2S,7S,8S,9S)-3,3,7-trimethyl-8-tricyclo[5.4.0.02,9]undecanyl]propanoic acid288412: Inhibition of human UGT2B7 assessed as reduction of estriol glucuronidationic500.9000uM
3-[(1R,2S,7R,8S,9R)-3,3,7-trimethyl-8-tricyclo[5.4.0.02,9]undecanyl]propan-1-ol288412: Inhibition of human UGT2B7 assessed as reduction of estriol glucuronidationic500.9000uM
(3S)-3-hydroxy-3-[(1R,2S,7S,8S,9S)-3,3,7-trimethyl-8-tricyclo[5.4.0.02,9]undecanyl]propanoic acid288412: Inhibition of human UGT2B7 assessed as reduction of estriol glucuronidationic501.0000uM
Mycophenolic Acid1223426: Uncompetitive substrate inhibition of UGT2B7 in non-diabetic human liver microsomes assessed as reduction in enzyme-mediated mycophenolic acid phenolic 7-O-glucuronide formation by HPLC and LC-MS/MS methodki1.5000uM
(1R,2S,7S,8S,9S)-3,3,7-trimethyltricyclo[5.4.0.02,9]undecane-8-carboxylic acid288412: Inhibition of human UGT2B7 assessed as reduction of estriol glucuronidationic502.0000uM
3-[(1R,2S,7R,8S,9R)-3,3,7-trimethyl-8-tricyclo[5.4.0.02,9]undecanyl]propanoic acid288412: Inhibition of human UGT2B7 assessed as reduction of estriol glucuronidationic502.0000uM
4-[(1R,2S,7R,8S,9R)-3,3,7-trimethyl-8-tricyclo[5.4.0.02,9]undecanyl]butan-1-ol288412: Inhibition of human UGT2B7 assessed as reduction of estriol glucuronidationic503.0000uM
(Z)-3-[(1R,2S,7S,8S,9S)-3,3,7-trimethyl-8-tricyclo[5.4.0.02,9]undecanyl]prop-2-enoic acid288412: Inhibition of human UGT2B7 assessed as reduction of estriol glucuronidationic503.0000uM
(E)-3-[(1R,2S,7S,8S,9S)-3,3,7-trimethyl-8-tricyclo[5.4.0.02,9]undecanyl]prop-2-enoic acid288412: Inhibition of human UGT2B7 assessed as reduction of estriol glucuronidationic503.0000uM
(1R)-3-dimethoxyphosphoryl-1-[(1R,2S,7S,8S,9S)-3,3,7-trimethyl-8-tricyclo[5.4.0.02,9]undecanyl]propan-1-ol288412: Inhibition of human UGT2B7 assessed as reduction of estriol glucuronidationic503.0000uM
(1S)-3-diethoxyphosphoryl-1-[(1R,2R,7S,8S,9S)-3,3,7-trimethyl-8-tricyclo[5.4.0.02,9]undecanyl]propan-1-ol288412: Inhibition of human UGT2B7 assessed as reduction of estriol glucuronidationic504.0000uM
(1S)-3-dimethoxyphosphoryl-1-[(1R,2S,7S,8S,9S)-3,3,7-trimethyl-8-tricyclo[5.4.0.02,9]undecanyl]propan-1-ol288412: Inhibition of human UGT2B7 assessed as reduction of estriol glucuronidationic504.0000uM
(1R)-3-diethoxyphosphoryl-1-[(1R,2R,7S,8S,9S)-3,3,7-trimethyl-8-tricyclo[5.4.0.02,9]undecanyl]propan-1-ol288412: Inhibition of human UGT2B7 assessed as reduction of estriol glucuronidationic505.0000uM
N,N-dimethyl-2-[(1R,2S,7R,8S,9R)-3,3,7-trimethyl-8-tricyclo[5.4.0.02,9]undecanyl]ethanamine;hydrochloride288412: Inhibition of human UGT2B7 assessed as reduction of estriol glucuronidationic505.0000uM
[(E)-2-[(1R,2S,7S,8R,9S)-3,3,7-trimethyl-8-tricyclo[5.4.0.02,9]undecanyl]ethenyl]phosphonic acid288412: Inhibition of human UGT2B7 assessed as reduction of estriol glucuronidationic508.0000uM
(1R)-2-diethoxyphosphoryl-1-[(1R,2R,7S,8S,9S)-3,3,7-trimethyl-8-tricyclo[5.4.0.02,9]undecanyl]ethanol288412: Inhibition of human UGT2B7 assessed as reduction of estriol glucuronidationic5010.0000uM
(1S)-2-diethoxyphosphoryl-1-[(1R,2S,7S,8S,9S)-3,3,7-trimethyl-8-tricyclo[5.4.0.02,9]undecanyl]ethanol288412: Inhibition of human UGT2B7 assessed as reduction of estriol glucuronidationic5010.0000uM

CTD chemical–gene interactions

176 total (human), top 30 by PubMed support.

ChemicalActions (top 5)PubMed papers
Diclofenacdecreases reaction, increases glucuronidation, affects glucuronidation, increases chemical synthesis, affects chemical synthesis (+4 more)10
Morphineaffects metabolic processing, increases glucuronidation6
hyodeoxycholic acidaffects metabolic processing, increases glucuronidation, increases glycosylation, affects cotreatment, increases metabolic processing5
Indomethacindecreases reaction, increases chemical synthesis, increases glucuronidation5
Ketoprofendecreases reaction, increases chemical synthesis, increases glucuronidation5
Naproxenincreases glucuronidation, decreases reaction, increases chemical synthesis5
Valproic Aciddecreases activity, decreases expression, decreases methylation, increases methylation, increases glucuronidation5
Zidovudinedecreases activity, decreases glucuronidation, decreases reaction, increases glucuronidation, decreases expression (+2 more)5
Androsteronedecreases reaction, increases glucuronidation, increases chemical synthesis, decreases activity4
Ibuprofendecreases reaction, increases chemical synthesis, increases glucuronidation4
tiaprofenic acidincreases glucuronidation, decreases reaction, increases chemical synthesis3
perfluorooctane sulfonic aciddecreases expression, increases expression3
4-(methylnitrosamino)-1-(3-pyridyl)-1-butan-1-olaffects abundance, increases glucuronidation3
Carvedilolaffects glucuronidation, affects metabolic processing, increases glucuronidation3
Clofibric Aciddecreases reaction, increases response to substance, increases glucuronidation3
Diflunisaldecreases reaction, increases chemical synthesis, increases glucuronidation3
Estradiolincreases glucuronidation3
Fenoprofendecreases reaction, increases chemical synthesis, increases glucuronidation3
Hymecromoneincreases glucuronidation, increases chemical synthesis, increases activity, increases metabolic processing, decreases reaction3
Mefenamic Aciddecreases reaction, increases chemical synthesis, increases glucuronidation, increases metabolic processing, increases abundance3
Phenobarbitalaffects expression, decreases expression, increases expression3
Aflatoxin B1decreases methylation, increases expression3
2-hydroxyestriolincreases glucuronidation2
benoxaprofenaffects response to substance, increases glucuronidation2
4-(N-methyl-N-nitrosamino)-1-(3-pyridyl)-1-butanonedecreases glucuronidation, increases glucuronidation2
sodium arseniteincreases methylation, decreases expression2
zomepiracincreases glucuronidation2
perfluorooctanoic aciddecreases expression, increases expression2
oxazepam glucuronideincreases abundance, increases chemical synthesis2
4-hydroxyestroneincreases glucuronidation2

ChEMBL screening assays

192 unique, capped per target: 178 admet, 12 binding, 2 functional

Representative assays (with source publication via chembl_document):

Assay IDTypeDescriptionSource paper
CHEMBL1743334ADMETSubstrate of human UDP-glucuronosyltransferase UGT2B7Casarett and Doull’s Toxicology The Basic Science of Poisons, 7th edition
CHEMBL1908123BindingDrug glucuronidation reaction catalyzed by human recombinant UGT2B7UDP-glucuronosyltransferases and clinical drug-drug interactions. — Pharmacol Ther
CHEMBL869545FunctionalCompetitive inhibition of UGT2B7-catalyzed scopoletin glucuronidationStereochemical sensitivity of the human UDP-glucuronosyltransferases 2B7 and 2B17. — J Med Chem

Clinical trials (associated diseases)

0 trials via MONDO — disease-level, not drug-specific.

No linked Atlas pages yet — the cross-entity mesh grows as the corpus expands.

About this page

Generated deterministically by Sugi Atlas from primary biomedical databases via BioBTree. Every record on this page traces to a primary source.

Generated
Atlas version
v1.1.4
BioBTree
v2.0.2

Sources 80

This page pulls from 80 datasets indexed by BioBTree:

alphafoldalphamissenseantibodybgeebgee_evidencebindingdbbiogrid_interactionbrendabrenda_kineticsccdscellosauruschembl_activitychembl_assaychembl_documentchembl_moleculechembl_targetciviccivic_evidenceclingen_dosageclingen_gene_validityclinical_trialsclinvarcollectrictd_gene_interactiondbsnpdepmapdiamond_similarityefoensemblentrezesm2_similarityexonfantom5_genefantom5_promotergenccgenerifgogoparentgtopdbgwasgwas_studyhgnchpointactinterprointogenjasparmeshmimmirdbmondomsigdborphanetorthologparalogpatentpatent_compoundpdbpfampharmgkb_clinicalpharmgkb_genepharmgkb_guidelinepharmgkb_variantpubchempubchem_activitypubchem_assaypubmedreactomereactomeparentrefseqrhearnacentralscxa_expressionscxa_gene_experimentsignorspliceaistring_interactiontranscriptufeatureuniprot