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Atlas / Gene / CES2

CES2

gene
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Also known as CE-2iCECES2A1

Summary

CES2 (carboxylesterase 2, HGNC:1864) is a protein-coding gene on chromosome 16q22.1, encoding Cocaine esterase (O00748). Involved in the detoxification of xenobiotics and in the activation of ester and amide prodrugs.

This gene encodes a member of the carboxylesterase large family. The family members are responsible for the hydrolysis or transesterification of various xenobiotics, such as cocaine and heroin, and endogenous substrates with ester, thioester, or amide bonds. They may participate in fatty acyl and cholesterol ester metabolism, and may play a role in the blood-brain barrier system. The protein encoded by this gene is the major intestinal enzyme and functions in intestine drug clearance. Alternatively spliced transcript variants have been found for this gene.

Source: NCBI Gene 8824 — RefSeq curated summary.

At a glance

  • Clinical variants (ClinVar): 88 total
  • Druggable target: yes — 5 molecules with ChEMBL bioactivity
  • MANE Select transcript: NM_001365405

Identifiers

Gene identifiers

FieldValue
HGNC IDHGNC:1864
Approved symbolCES2
Namecarboxylesterase 2
Location16q22.1
Locus typegene with protein product
StatusApproved
AliasesCE-2, iCE, CES2A1
Ensembl geneENSG00000172831
Ensembl biotypeprotein_coding
OMIM605278
Entrez8824

Gene structure

Transcript identifiers

Ensembl transcripts: 21 — 13 protein_coding, 5 retained_intron, 2 nonsense_mediated_decay, 1 protein_coding_CDS_not_defined

ENST00000317091, ENST00000417689, ENST00000561697, ENST00000561843, ENST00000563988, ENST00000564420, ENST00000566182, ENST00000566359, ENST00000567128, ENST00000568347, ENST00000568470, ENST00000570032, ENST00000885060, ENST00000885061, ENST00000885062, ENST00000971760, ENST00000971761, ENST00000971762, ENST00000971763, ENST00000971764, ENST00000971765

RefSeq mRNA: 6 — MANE Select: NM_001365405 NM_001365405, NM_001365406, NM_001365407, NM_001365408, NM_003869, NM_198061

CCDS: CCDS10825, CCDS45507

Canonical transcript exons

ENST00000317091 — 12 exons

ExonStartEnd
ENSE000017294046694383966945096
ENSE000019437136693551666935711
ENSE000034695866693803766938241
ENSE000034746856694043766940695
ENSE000034948156694022266940355
ENSE000034977586694150666941646
ENSE000035197656693921766939358
ENSE000035764566694210566942249
ENSE000035938816694176866941848
ENSE000036390796694264866942785
ENSE000036698986694112466941222
ENSE000036845716694329966943371

Expression profiles

Bgee: expression breadth ubiquitous, 293 present calls, max score 99.88.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 17.8461 / max 1208.4042, expressed in 1812 samples.

FANTOM5 promoters (6 alternative TSS)

Promoter IDTPM avgSamples expressed
15453612.68791811
1545392.0270328
1545401.8222133
1545370.7881566
1545380.2614116
1545350.259598

Top tissues by expression

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

TissueAnatomy IDExpression scoreQuality
jejunal mucosaUBERON:000039999.88gold quality
ileal mucosaUBERON:000033199.77gold quality
colonic mucosaUBERON:000031799.64gold quality
mucosa of sigmoid colonUBERON:000499399.64gold quality
duodenumUBERON:000211499.29gold quality
tongue squamous epitheliumUBERON:000691999.28gold quality
mucosa of transverse colonUBERON:000499199.10gold quality
pharyngeal mucosaUBERON:000035598.89gold quality
rectumUBERON:000105298.67gold quality
lower esophagus mucosaUBERON:003583498.61gold quality
right lobe of liverUBERON:000111498.41gold quality
nephron tubuleUBERON:000123198.38gold quality
esophagus squamous epitheliumUBERON:000692098.16gold quality
esophagus mucosaUBERON:000246998.15gold quality
epithelium of esophagusUBERON:000197698.07gold quality
liverUBERON:000210797.82gold quality
kidney epitheliumUBERON:000481997.50gold quality
left ventricle myocardiumUBERON:000656697.47gold quality
squamous epitheliumUBERON:000691497.34gold quality
small intestineUBERON:000210897.23gold quality
cervix squamous epitheliumUBERON:000692297.21gold quality
pancreatic ductal cellCL:000207997.13gold quality
small intestine Peyer’s patchUBERON:000345497.07gold quality
heart right ventricleUBERON:000208097.01gold quality
body of tongueUBERON:001187696.91gold quality
jejunumUBERON:000211596.87gold quality
oral cavityUBERON:000016796.72gold quality
renal glomerulusUBERON:000007496.56gold quality
transverse colonUBERON:000115796.48gold quality
renal medullaUBERON:000036296.47gold quality

Single-cell (SCXA)

Detected in 3 experiment(s), a significant marker in 2.

ExperimentMarker?Max mean expression
E-GEOD-125970yes1655.85
E-ENAD-17no213.42
E-ANND-3no0.00

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

46 targeting CES2, 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-6873-3P100.0071.422626
HSA-MIR-4455100.0065.481587
HSA-MIR-432-3P100.0067.86705
HSA-MIR-7110-3P100.0073.182486
HSA-MIR-548C-3P99.9974.017587
HSA-MIR-335-3P99.9373.364958
HSA-MIR-129799.9173.413162
HSA-MIR-4753-3P99.9071.033786
HSA-MIR-26A-5P99.7873.522303
HSA-MIR-26B-5P99.7873.512305
HSA-MIR-4446-5P99.7269.192544
HSA-MIR-1296-3P99.7264.04636
HSA-MIR-4755-5P99.7170.342716
HSA-MIR-5006-3P99.7170.262728
HSA-MIR-444199.4966.563216
HSA-MIR-1207-5P99.4969.112983
HSA-MIR-468899.4864.68828
HSA-MIR-130A-5P99.3370.262623
HSA-MIR-6734-3P99.1566.271627
HSA-MIR-4763-3P99.1067.832649
HSA-MIR-29A-5P99.0868.591813
HSA-MIR-6506-5P99.0465.661386
HSA-MIR-427099.0266.261987
HSA-MIR-125798.9768.021133
HSA-MIR-471098.6165.961048
HSA-MIR-6754-5P98.6065.541627
HSA-MIR-619-5P98.5764.971988
HSA-MIR-6887-5P98.5668.491295
HSA-MIR-3928-5P98.5067.48980
HSA-MIR-6806-3P98.5067.31980

Literature-anchored findings (GeneRIF, showing 40)

  • The multiple promoters in the CES2 gene were characterized. (PMID:12835618)
  • Single-nucleotide polymorphism in carboxylesterase 2 is associated with reduced mRNA expression in colorectal tumors (PMID:15475243)
  • analysis of single nucleotide polymorphisms and haplotype structure of the human carboxylesterase 2 gene (PMID:15475733)
  • human carboxylesterase 2 gene presents several polymorphisms, none of which seems to be involved in significant variations in protein activity (PMID:15592324)
  • TFF-1 is lost late in the progression from Barrett’s Esophagus to adenocarcinoma, while CES-2 is upregulated (PMID:15967118)
  • in diffuse large B-cell lymphoma, molecular alterations in ice, bcl-2, c-myc and p53 are present in hematopoietic cells from bone marrow as well as in primitive hematopoietic progenitors (PMID:16690525)
  • p53 directly regulates CES-2 expression in a colonic cancer cell line. (PMID:16963839)
  • 830C>G single nucleotide polymorphism of CES2 is unlikely to have significant functional consequences on CES2 expression, activity or function (PMID:17483951)
  • IL-6 alters the cellular responsiveness to clopidogrel, irinotecan, and oseltamivir by suppressing the expression of CES2. (PMID:17537833)
  • In a Japanese population, CES2 haplotypes and a defective allele were associated with a decrease in enzyme levels or activity. Pharmacokinetics of irinotecan was evaluated in cancer patients. (PMID:17640957)
  • comparative analysis of CES1 and CES2 in liver and small intestine of humans, monkeys, dogs, rabbits and rats (PMID:17764701)
  • Carboxylesterase 2 is downregulated in colorectal cancer following progression of the disease (PMID:18259949)
  • Carboxylesterase 1A2 has been isolated and determined to be identical to carboxylesterase 1A1 except for exon 1 and the 5’ regulatory element. (PMID:18305377)
  • an association between a polymorphism in the CES2 gene and the efficacy of capecitabine has been described (PMID:18473752)
  • pharmacogenomic characterization of human carboxylesterase 1A1, 1A2, and 1A3 genes (PMID:18794728)
  • Carboxylesterases play critical roles in drug metabolism and insecticide detoxication; findings show large variability among different age groups or even within the same age group. (PMID:18983829)
  • A comparison of the substrate specificity of CES1 versus CES2 reveals broad but distinct substrate preferences. (PMID:19508181)
  • serum carboxylesterase-2 level might be a potential marker in the diagnosis of the early stage ovarian cancer. (PMID:19856659)
  • Report CES2 mediated hydrolysis of heroin, cocaine and CPT-11. (PMID:20649590)
  • tested the hypothesis that an individual’s CES phenotype can be characterized by reporter substrates/probes that interrogate native CES1 and CES2 activities in liver and immunoblotting methods (PMID:22525521)
  • Variations in CES2 in the promoter region, may alter rifampicin metabolism by affecting expression of the gene (PMID:23471941)
  • CES2 RNA expression was observed in neuroblastoma cells, and its expression in neuroblastoma cell lines was positively correlated with sensitivity to CPT-11 and apoptosis after CPT-11 exposure in vitro (PMID:23480903)
  • expression of CES2, UGTA1A1, and GUSB varies in colorectal pathology tissues and that the expression of CES2 is somewhat related to tumor staging. (PMID:24195516)
  • After oral administration of dabigatran etexilate to humans, DABE is hydrolyzed by intestinal CES2 to the intermediate M2 metabolite followed by hydrolysis of M2 to DAB in the liver by CES1. (PMID:24212379)
  • In the liver and duodenum, CES2 mRNA expression increased and exhibited a postnatal surge. (PMID:25724353)
  • Findings suggest that CES2 expression and activity, by mediating the intratumoral activation of irinotecan, is a contributor to FOLFIRINOX sensitivity in pancreatic cancer. (PMID:26025324)
  • has triglyceride hydrolase activity; as a result, gain of hepatic CES2 function increases fatty acid oxidation and inhibits lipogenesis, whereas loss of hepatic CES2 stimulates lipogenesis by inducing endoplasmic reticulum stress (PMID:26806650)
  • These data suggest that infants younger than 3 weeks of age would exhibit significantly lower CES1- and CES2-dependent metabolic clearance compared with older individuals. (PMID:26825642)
  • Plasma cells are strong producers of CES-2 in intestinal inflammation and cancer and may be involved in metabolic activation of ester-containing prodrugs. (PMID:27149931)
  • Carboxylesterase 2 possesses triglyceride and diacylglycerol lipase activities and displayed an inverse correlation with HOMA-IR and hepatic diacylglycerol concentrations in humans. (PMID:28099843)
  • Data show that carboxylesterase 2 (CES2A1) is the primary mediator of carboxylesterase (CES) substrates in the enterocytes. (PMID:28285137)
  • Anordrin is predominantly catalyzed by CES1 and CES2 to generate the main active metabolite, anordiol. (PMID:28532270)
  • SNPs in CDA and CES2 were associated with benefit from the addition of capecitabine to chemotherapy in metastatic breast cancer patients. (PMID:28827188)
  • High expression of TOPO-1 and CES-2 are correlated with longer progression free and overall survival in irinotecan treated metastatic colorectal cancer patients. (PMID:29261002)
  • Effect of genetic variation of NAT2 on isoniazid and SLCO1B1 and CES2 on rifampin pharmacokinetics in Ghanaian children with tuberculosis has been reported. (PMID:29263072)
  • Results revealed that most of the colorectal cancer specimens showed a considerable reduction in CES2 expression compared with adjacent normal tissue independently of p53. (PMID:29651325)
  • This study showed for the first time that CE-2 activity was much lower in breast cancer cells than in normal cells. (PMID:30016861)
  • The T/T genotype of the polymorphism rs2241409 in CES2 gene is associated with graft rejection during kidney transplantation. (PMID:30442353)
  • Prognostic Impact of Carboxylesterase 2 in Cholangiocarcinoma. (PMID:30867471)
  • Identification and Characterization of a New Carboxylesterase 2 Isozyme, mfCES2C, in the Small Intestine of Cynomolgus Monkeys. (PMID:31836607)

Cross-species orthologs

70 orthologs

OrganismSymbolGene ID
danio_rerioces2aENSDARG00000041569
danio_rerioces3ENSDARG00000041595
danio_reriosi:ch73-89b15.3ENSDARG00000053709
danio_reriosi:dkey-30c15.17ENSDARG00000058492
danio_rerionlgn3bENSDARG00000062376
danio_rerionlgn2bENSDARG00000079251
danio_reriosi:ch211-71n6.4ENSDARG00000102234
mus_musculusCes2gENSMUSG00000031877
mus_musculusCes2eENSMUSG00000031886
mus_musculusCes2bENSMUSG00000050097
mus_musculusCes2aENSMUSG00000055730
mus_musculusCes2cENSMUSG00000061825
mus_musculusCes2fENSMUSG00000062826
rattus_norvegicusCes2jENSRNOG00000011330
rattus_norvegicusCes2eENSRNOG00000011635
rattus_norvegicusCes2iENSRNOG00000012034
rattus_norvegicusCes2gENSRNOG00000013808
rattus_norvegicusCes2jENSRNOG00000029744
rattus_norvegicusCes2cENSRNOG00000036571
rattus_norvegicusCes2bENSRNOG00000048039
rattus_norvegicusLOC679368ENSRNOG00000048823
rattus_norvegicusCes2c-ps2ENSRNOG00000052151
rattus_norvegicusCes2fENSRNOG00000069933
rattus_norvegicusCes2gENSRNOG00000070043
drosophila_melanogasterEst-6FBGN0000592
drosophila_melanogasterEst-PFBGN0000594
drosophila_melanogasterGltFBGN0001114
drosophila_melanogasterGliFBGN0001987
drosophila_melanogasterJheFBGN0010052
drosophila_melanogasteralpha-Est1FBGN0015568
drosophila_melanogasteralpha-Est10FBGN0015569
drosophila_melanogasteralpha-Est2FBGN0015570
drosophila_melanogasteralpha-Est3FBGN0015571
drosophila_melanogasteralpha-Est4FBGN0015572
drosophila_melanogasteralpha-Est6FBGN0015574
drosophila_melanogasteralpha-Est7FBGN0015575
drosophila_melanogasteralpha-Est8FBGN0015576
drosophila_melanogasteralpha-Est9FBGN0015577
drosophila_melanogasterCG4757FBGN0027584
drosophila_melanogasterCG9287FBGN0032057
drosophila_melanogasterCG9289FBGN0032058
drosophila_melanogasterCG3841FBGN0032131
drosophila_melanogasterCG4382FBGN0032132
drosophila_melanogasterJhedupFBGN0034076
drosophila_melanogastergasFBGN0034736
drosophila_melanogasterNlg3FBGN0083963
drosophila_melanogasteralpha-Est5FBGN0261393
caenorhabditis_elegansWBGENE00000037
caenorhabditis_elegansWBGENE00000038
caenorhabditis_elegansWBGENE00001578
caenorhabditis_elegansWBGENE00006412
caenorhabditis_elegansWBGENE00007691
caenorhabditis_elegansWBGENE00007692
caenorhabditis_elegansWBGENE00007693
caenorhabditis_elegansWBGENE00007695
caenorhabditis_elegansWBGENE00008451
caenorhabditis_elegansWBGENE00011362
caenorhabditis_elegansWBGENE00011364
caenorhabditis_elegansWBGENE00013873
caenorhabditis_elegansWBGENE00013874
caenorhabditis_elegansWBGENE00013875
caenorhabditis_elegansWBGENE00015067
caenorhabditis_elegansWBGENE00015071
caenorhabditis_elegansWBGENE00015279
caenorhabditis_elegansWBGENE00015284
caenorhabditis_elegansWBGENE00016595
caenorhabditis_elegansWBGENE00016862
caenorhabditis_elegansWBGENE00016863
caenorhabditis_eleganscest-27WBGENE00018958
caenorhabditis_elegansWBGENE00020688

Paralogs (13): TG (ENSG00000042832), ACHE (ENSG00000087085), BCHE (ENSG00000114200), NLGN4X (ENSG00000146938), CES5A (ENSG00000159398), NLGN4Y (ENSG00000165246), NLGN1 (ENSG00000169760), NLGN2 (ENSG00000169992), CEL (ENSG00000170835), CES4A (ENSG00000172824), CES3 (ENSG00000172828), NLGN3 (ENSG00000196338), CES1 (ENSG00000198848)

Protein

Protein identifiers

Cocaine esterase — O00748 (reviewed: O00748)

Alternative names: Carboxylesterase 2, Methylumbelliferyl-acetate deacetylase 2

All UniProt accessions (4): O00748, H3BUN5, J3QLP1, J3QSC0

UniProt curated annotations — full annotation on UniProt →

Function. Involved in the detoxification of xenobiotics and in the activation of ester and amide prodrugs. Shows high catalytic efficiency for hydrolysis of cocaine, 4-methylumbelliferyl acetate, heroin and 6-monoacetylmorphine. Hydrolyzes aspirin, substrates with large alcohol group and small acyl group and endogenous lipids such as triacylglycerol. Converts monoacylglycerides to free fatty acids and glycerol. Hydrolyzes of 2-arachidonoylglycerol and prostaglandins.

Subunit / interactions. Monomer.

Subcellular location. Endoplasmic reticulum lumen.

Tissue specificity. Preferentially expressed in intestine with moderate expression in liver. Within the intestine, highest expression is found in small intestine with lower expression in colon and rectum.

Post-translational modifications. Glycosylated.

Miscellaneous. Probably produced by alternative initiation of isoform 1. Does not contain a signal peptide. The biological function of the extra amino acids in the N-terminus remains to be determined. Probably produced by alternative initiation of isoform 2. Does not contain a signal peptide. The biological function of the extra amino acids in the N-terminus remains to be determined.

Similarity. Belongs to the type-B carboxylesterase/lipase family.

Isoforms (4)

UniProt IDNamesCanonical?
O00748-11yes
O00748-22
O00748-43
O00748-54

RefSeq proteins (6): NP_001352334, NP_001352335, NP_001352336, NP_001352337, NP_003860, NP_932327 (=MANE)

Domains & families (InterPro)

IDNameType
IPR002018CarbesteraseBDomain
IPR019819Carboxylesterase_B_CSConserved_site
IPR019826Carboxylesterase_B_ASActive_site
IPR029058AB_hydrolase_foldHomologous_superfamily
IPR050309Type-B_Carboxylest/LipaseFamily

Pfam: PF00135

Enzyme classification (BRENDA):

  • EC 3.1.1.1 — carboxylesterase (BRENDA: 126 organisms, 1207 substrates, 1167 inhibitors, 834 Km, 540 kcat entries)
  • EC 3.1.1.84 — cocaine esterase (BRENDA: 4 organisms, 26 substrates, 4 inhibitors, 65 Km, 53 kcat entries)

Substrate kinetics (BRENDA)

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

SubstrateKm (mM)Measurements
4-NITROPHENYL ACETATE0.013–4.4761
4-NITROPHENYL HEXANOATE0.004–44.741
4-NITROPHENYL BUTYRATE0.0004–1.639
4-NITROPHENYL BUTANOATE0.004–12732
4-NITROPHENYL OCTANOATE0.0117–25.231
4-NITROPHENYL DODECANOATE0.0008–67.626
4-NITROPHENYL PROPIONATE0.0338–3.318
4-NITROPHENYL PENTANOATE0.02–2.114
4-NITROPHENYL DECANOATE0.008–4.9913
4-NITROPHENYL HEXADECANOATE0.005–4.812
4-YETHYLUMBELLIFERYL ACETATE0.022–29
7-ETHYL-10-[4-(1-PIPERIDINO)-1-AMINO]CARBONYLOXY0.0555–0.08519
CPT-1158.05–81.019
1-NAPHTHYL ACETATE0.008–1.018
4-NITROPHENYL CAPROATE0.008–3.88

Catalyzed reactions (Rhea), 6 shown:

  • 4-methylumbelliferyl acetate + H2O = 4-methylumbelliferone + acetate + H(+) (RHEA:12208)
  • a carboxylic ester + H2O = an alcohol + a carboxylate + H(+) (RHEA:21164)
  • 2-(5Z,8Z,11Z,14Z-eicosatetraenoyl)-glycerol + H2O = glycerol + (5Z,8Z,11Z,14Z)-eicosatetraenoate + H(+) (RHEA:26132)
  • cocaine + H2O = ecgonine methyl ester + benzoate + H(+) (RHEA:27506)
  • prostaglandin E2 1-glyceryl ester + H2O = prostaglandin E2 + glycerol + H(+) (RHEA:48296)
  • prostaglandin F2alpha 1-glyceryl ester + H2O = prostaglandin F2alpha + glycerol + H(+) (RHEA:48300)

UniProt features (20 total): sequence conflict 5, active site 3, disulfide bond 2, splice variant 2, sequence variant 2, glycosylation site 2, signal peptide 1, chain 1, short sequence motif 1, modified residue 1

Structure

Experimental structures (PDB)

0 structures.

Predicted structure (AlphaFold)

ModelpLDDTFraction very-high
AF-O00748-F190.960.78

Functional residue map

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

Catalytic / active sites (3): 228 (acyl-ester intermediate); 345 (charge relay system); 457 (charge relay system)

Post-translational modifications (1): 27

Disulfide bonds (2): 280–291, 95–123

Glycosylation sites (2): 111, 276

Function

Pathways and Gene Ontology

Reactome pathways

2 pathways

IDPathway
R-HSA-211945Phase I - Functionalization of compounds
R-HSA-9749641Aspirin ADME

MSigDB gene sets: 172 (showing top): REACTOME_BIOLOGICAL_OXIDATIONS, CHIARADONNA_NEOPLASTIC_TRANSFORMATION_KRAS_DN, chr16q22, YAO_HOXA10_TARGETS_VIA_PROGESTERONE_UP, GNF2_GSTM1, GNF2_HPN, GRAESSMANN_APOPTOSIS_BY_DOXORUBICIN_UP, GRAESSMANN_RESPONSE_TO_MC_AND_DOXORUBICIN_UP, IVANOVA_HEMATOPOIESIS_LATE_PROGENITOR, GOBP_REGULATION_OF_HORMONE_LEVELS, HSIAO_HOUSEKEEPING_GENES, GOBP_RETINOL_METABOLIC_PROCESS, GOBP_MONOCARBOXYLIC_ACID_METABOLIC_PROCESS, SHETH_LIVER_CANCER_VS_TXNIP_LOSS_PAM1, SHETH_LIVER_CANCER_VS_TXNIP_LOSS_PAM3

GO Biological Process (7): prostaglandin metabolic process (GO:0006693), xenobiotic metabolic process (GO:0006805), cocaine catabolic process (GO:0050784), morphine catabolic process (GO:0071273), detoxification (GO:0098754), lipid metabolic process (GO:0006629), catabolic process (GO:0009056)

GO Molecular Function (4): methylumbelliferyl-acetate deacetylase activity (GO:0047374), carboxylic ester hydrolase activity (GO:0052689), carboxylesterase activity (GO:0106435), hydrolase activity (GO:0016787)

GO Cellular Component (2): endoplasmic reticulum (GO:0005783), endoplasmic reticulum lumen (GO:0005788)

Reactome top-level categories

Rollup of top-2 pathways:

CategoryPathways
Biological oxidations1
Drug ADME1

GO top-level categories

Rollup of top GO terms by namespace:

CategoryTerms
metabolic process2
carboxylic ester hydrolase activity2
prostanoid metabolic process1
cellular response to xenobiotic stimulus1
alkaloid catabolic process1
morphine metabolic process1
isoquinoline alkaloid catabolic process1
biological_process1
response to toxic substance1
primary metabolic process1
deacetylase activity1
hydrolase activity, acting on ester bonds1
catalytic activity1
cytoplasm1
endomembrane system1
intracellular membrane-bounded organelle1
endoplasmic reticulum1
intracellular organelle lumen1

Protein interactions and networks

STRING

856 interactions, top by confidence (×1000):

Protein AProtein BPartner UniProtScore
CES2ESDP10768868
CES2HAGHQ16775765
CES2ADH5P11766694
CES2AADACP22760606
CES2UGT1A1P22309583
CES2UGT1A7Q9HAW7583
CES2UGT1A6P19224582
CES2CD2P06729569
CES2ALBP02768557
CES2UGT1A10Q9HAW8553
CES2UGT1A4P22310553
CES2UGT1A8Q9HAW9553
CES2CYP3A4P05184518
CES2LTFP02788448
CES2UGT2B7P16662434

IntAct

125 interactions, top by confidence:

ABTypeScore
CES2MAST2psi-mi:“MI:0407”(direct interaction)0.440
CES2PDZD2psi-mi:“MI:0407”(direct interaction)0.440
CES2ARHGEF12psi-mi:“MI:0407”(direct interaction)0.440
CES2PTPN3psi-mi:“MI:0407”(direct interaction)0.440
CES2SNTB1psi-mi:“MI:0407”(direct interaction)0.440
CES2SCRIBpsi-mi:“MI:0407”(direct interaction)0.440
CES2SNX27psi-mi:“MI:0407”(direct interaction)0.440
CES2PDZK1psi-mi:“MI:0407”(direct interaction)0.440
CES2PDZD7psi-mi:“MI:0407”(direct interaction)0.440
SNTA1CES2psi-mi:“MI:0407”(direct interaction)0.440
CES2ARHGEF11psi-mi:“MI:0407”(direct interaction)0.440
CES2NHERF2psi-mi:“MI:0407”(direct interaction)0.440
TAMALINCES2psi-mi:“MI:0407”(direct interaction)0.440
SHANK1CES2psi-mi:“MI:0407”(direct interaction)0.440
PDZK1CES2psi-mi:“MI:0407”(direct interaction)0.440
CES2GRID2IPpsi-mi:“MI:0407”(direct interaction)0.440
CES2MAGI2psi-mi:“MI:0407”(direct interaction)0.440
CES2DLG3psi-mi:“MI:0407”(direct interaction)0.440
CES2HTRA1psi-mi:“MI:0407”(direct interaction)0.440
CES2RHPN1psi-mi:“MI:0407”(direct interaction)0.440
CES2SYNJ2BPpsi-mi:“MI:0407”(direct interaction)0.440
CES2PDZRN3psi-mi:“MI:0407”(direct interaction)0.440
CES2DLG1psi-mi:“MI:0407”(direct interaction)0.440
CES2PDZRN4psi-mi:“MI:0407”(direct interaction)0.440
CES2NHERF4psi-mi:“MI:0407”(direct interaction)0.440
TIAM2CES2psi-mi:“MI:0407”(direct interaction)0.440
CES2FRMPD4psi-mi:“MI:0407”(direct interaction)0.440
CES2DLG4psi-mi:“MI:0407”(direct interaction)0.440

BioGRID (32): CES2 (Affinity Capture-MS), CES2 (Proximity Label-MS), ANKRD9 (Affinity Capture-MS), SNTG1 (Affinity Capture-MS), CRELD1 (Affinity Capture-MS), SERPINF2 (Affinity Capture-MS), STIM1 (Affinity Capture-MS), HIBADH (Affinity Capture-MS), PI4K2A (Affinity Capture-MS), PNMAL1 (Affinity Capture-MS), SLC22A4 (Affinity Capture-MS), CES2 (Affinity Capture-MS), ARHGEF1 (Affinity Capture-MS), CES2 (Affinity Capture-MS), TRIP10 (Affinity Capture-MS)

ESM2 similar proteins: A0A0B4K692, A0A6J2ATK2, B2RQR8, D0G895, F1N476, F1RRW5, M3XFH7, O00748, O16796, O44857, O95672, P07861, P08049, P08473, P09470, P0C1T0, P0DPD6, P0DPD8, P0DPD9, P0DPE2, P12820, P12821, P12822, P23276, P42891, P42892, P42893, P47820, P97739, Q07075, Q18673, Q22523, Q495T6, Q4PZA2, Q50JE5, Q5RCL7, Q5RE69, Q61391, Q6AW47, Q6UWW8

Diamond homologs: A0A060S684, A0A0E4AET8, A0A8B0RBM2, B0F2B4, D2D3B6, D6WMZ8, G3V7J5, I1RDA9, O00748, O16168, O16169, O16170, O16171, O16172, O16173, O42275, O46421, O62760, O62761, O70631, P04058, P06276, P07882, P08171, P0C6R3, P10959, P12337, P12992, P14943, P16303, P16854, P18142, P19835, P21837, P21927, P23141, P23953, P25725, P25726, P25727

SIGNOR signaling

0 interactions.

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 83 IntAct physical interaction partners (hypergeometric vs the genome-wide background, BH-FDR, gene-set size 15–500, ranked by fold). A functional readout of the neighbourhood — distinct from this gene’s own memberships above, and biased toward well-studied / hub proteins, so read it as themes rather than proof.

Reactome pathways:

PathwayPartnersFoldFDR
Assembly and cell surface presentation of NMDA receptors732.3×3e-07
Neurexins and neuroligins932.2×2e-09
Protein-protein interactions at synapses629.0×6e-06
RHOB GTPase cycle514.0×1e-03
RHOC GTPase cycle513.3×1e-03
RHOA GTPase cycle68.1×2e-03
Extracellular matrix organization66.9×4e-03

GO biological processes:

GO termPartnersFoldFDR
establishment or maintenance of epithelial cell apical/basal polarity751.5×4e-08
protein localization to synapse548.5×1e-05
receptor clustering539.5×2e-05
regulation of postsynaptic membrane neurotransmitter receptor levels637.6×3e-06
protein-containing complex assembly811.5×6e-05
cell-cell adhesion810.3×9e-05
regulation of small GTPase mediated signal transduction59.1×7e-03

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

ClassificationCount (floor)
Pathogenic0
Likely pathogenic0
Uncertain significance66
Likely benign8
Benign1

Top pathogenic / likely-pathogenic (0)

SpliceAI

0 predictions. Top by Δscore:

AlphaMissense

3686 scored. Top likely-pathogenic:

VariantProtein changeam_pathogenicity
16:66938132:T:CF58L0.990
16:66938134:C:AF58L0.990
16:66938134:C:GF58L0.990
16:66938147:T:CF63L0.989
16:66938149:T:AF63L0.989
16:66938149:T:GF63L0.989
16:66940464:C:AN195K0.989
16:66940464:C:GN195K0.989
16:66940477:G:CD200H0.989
16:66940330:C:AR178S0.986
16:66940348:T:CF184L0.986
16:66940350:C:AF184L0.986
16:66940350:C:GF184L0.986
16:66940478:A:TD200V0.986
16:66940478:A:CD200A0.985
16:66940522:T:CF215L0.985
16:66940524:T:AF215L0.985
16:66940524:T:GF215L0.985
16:66940498:T:AW207R0.983
16:66940498:T:CW207R0.983
16:66940576:A:CS233R0.983
16:66940578:T:AS233R0.983
16:66940578:T:GS233R0.983
16:66939220:T:GC95W0.981
16:66940331:G:CR178P0.981
16:66940502:T:AV208D0.981
16:66939304:C:GC123W0.980
16:66940500:G:CW207C0.980
16:66940500:G:TW207C0.980
16:66940561:T:CS228P0.980

dbSNP variants (sampled 300 via entrez): RS1000406021 (16:66935881 C>CTCCTAGAA), RS1000633117 (16:66943481 T>C), RS1000741847 (16:66937157 A>G), RS1000822938 (16:66939633 C>A,T), RS1000967376 (16:66933369 A>C), RS1001207407 (16:66937856 G>C), RS1002254091 (16:66938634 A>C), RS1002291333 (16:66936730 C>T), RS1002353420 (16:66944941 C>T), RS1002606639 (16:66939020 C>T), RS1002764377 (16:66932782 G>A,C), RS1002826234 (16:66944582 A>G), RS1002876636 (16:66941276 G>A), RS1002905238 (16:66934168 T>C), RS1003158124 (16:66939942 A>G)

Disease associations

OMIM: gene MIM:605278 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

0 associations (top):

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL3180 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

5 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 146,776 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

MoleculeNamePhasePatents
CHEMBL806FLUTAMIDE499,079
CHEMBL841LOPERAMIDE422,587
CHEMBL1473252SODIUM TANSHINONE IIA SULFONATE2160
CHEMBL15192LAPACHONE2589
CHEMBL230006ENOXOLONE224,361

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

PharmGKB variants

2 variants.

VariantGenesLevelScore#Clin annotsDrugs
rs8192924CES20.000
rs11075646CES2, CIAO2B0.000

GtoPdb / IUPHAR curated pharmacology

(IUPHAR/BPS Guide to Pharmacology — expert-curated)

Target class: enzyme — Hydrolases & Lipases

Most potent curated ligand interactions (3 total), top 3:

LigandActionAffinityParameter
CES2 inhibitor 9dInhibition9.37pKi
tanshinone IIAInhibition7.16pKi
(+)-Yanhusanine BInhibition5.7pIC50

ChEMBL bioactivities

283 potent at pChembl≥5 of 333 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChemblTypeValueUnitMolecule
9.75IC500.1778nMCHEMBL155514
8.49Ki3.2nMCHEMBL193140
8.47IC503.388nMCHEMBL155513
8.39Ki4.1nMCHEMBL193140
8.39IC504.04nMCHEMBL4854298
8.36Ki4.4nMCHEMBL191847
8.36IC504.33nMCHEMBL4853742
8.30Ki4.98nMCHEMBL395018
8.26IC505.495nMCHEMBL153080
8.25Ki5.6nMCHEMBL362996
8.25Ki5.6nMCHEMBL5593400
8.24IC505.8nMCHEMBL89506
8.24Ki5.7nMCHEMBL1812859
8.16IC506.918nMCHEMBL440542
8.13IC507.4nMCHEMBL270373
8.10Ki7.9nMCHEMBL191847
8.07IC508.5nMCHEMBL89506
8.05Ki8.9nMCHEMBL191822
8.01Ki9.8nMCHEMBL362996
8.01IC509.84nMCHEMBL4858186
7.99Ki10.3nMCHEMBL192474
7.97IC5010.81nMCHEMBL4868014
7.96IC5011nMCHEMBL270373
7.87Ki13.6nMCHEMBL242931
7.83Ki14.7nMBENZIL
7.82Ki15nMBENZIL
7.82Ki15.1nMBENZIL
7.77IC5016.92nMCHEMBL4855838
7.77Ki17nMCHEMBL5569484
7.75IC5018nMCHEMBL5567105
7.74Ki18.2nMCHEMBL192180
7.73Ki18.6nMCHEMBL193228
7.70IC5020nMCHEMBL3774603
7.70IC5020nMCHEMBL86668
7.68IC5021nMCHEMBL273139
7.67Ki21.3nMCHEMBL192241
7.64Ki23nMCHEMBL193229
7.64Ki22.8nMCHEMBL192252
7.63Ki23.4nMCHEMBL193229
7.63IC5023.44nMCHEMBL4853637
7.62Ki24nMBENZIL
7.61Ki24.5nMCHEMBL1812859
7.59Ki25.9nMCHEMBL242067
7.59Ki25.7nMCHEMBL244631
7.59Ki25.6nMCHEMBL1812858
7.58Ki26nMCHEMBL1812858
7.58IC5026nMCHEMBL273139
7.56Ki27.5nMCHEMBL192139
7.54Ki28.7nMCHEMBL1812864
7.53Ki29.7nMCHEMBL192180

PubChem BioAssay actives

284 with measured affinity, of 670 total; 50 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.

CompoundAssayTypeValueUnit
1,1,1-trifluoro-3-hexylseleninylpropan-2-one48316: In vitro inhibition of carboxylesterase in human liver microsomes.ic500.0002uM
1-(3,4-dimethylphenyl)-2-phenylethane-1,2-dione239314: Inhibition constant against human intestinal carboxylesterase 2 using 4-MUA (4-methylumbelliferone acetate) as substrateki0.0032uM
1,1,1-trifluoro-3-hexylselenonylpropan-2-one48316: In vitro inhibition of carboxylesterase in human liver microsomes.ic500.0034uM
ethyl (Z)-4,4,4-trifluoro-3-hydroxy-2-[(2-nitrophenyl)diazenyl]but-2-enoate1762417: Inhibition of human recombinant CES2 expressed in mouse NSO cells using 4-NPA as substrate by spectrophotometric analysisic500.0040uM
ethyl (Z)-4,4,4-trifluoro-3-hydroxy-2-phenyldiazenylbut-2-enoate1762417: Inhibition of human recombinant CES2 expressed in mouse NSO cells using 4-NPA as substrate by spectrophotometric analysisic500.0043uM
1-(4-methyl-3-nitrophenyl)-2-phenylethane-1,2-dione239314: Inhibition constant against human intestinal carboxylesterase 2 using 4-MUA (4-methylumbelliferone acetate) as substrateki0.0044uM
1,2-bis(2,3-difluorophenyl)ethane-1,2-dione295501: Inhibition of human intestinal carboxylesteraseki0.0050uM
1,1,1-trifluoro-3-(hexylamino)propan-2-one48316: In vitro inhibition of carboxylesterase in human liver microsomes.ic500.0055uM
1-[4-(2-oxo-2-phenylacetyl)phenyl]-2-phenylethane-1,2-dione239272: Inhibition constant against human intestinal carboxylesterase 2 (hiCE) using nitrophenyl acetate (o-NPA) as substrateki0.0056uM
(6-methoxy-3-methyl-1-benzothiophen-2-yl)-piperidin-1-ylmethanone2099510: Competitive type of inhibition at human recombinant CES2 activity assessed as fluorescence of the AP product using Benz-AP as substrateki0.0056uM
octadecane-9,10-dione612131: Inhibition of human intestinal carboxylesterase using o-nitrophenyl acetate as substrate after 5 mins by spectrophotometryki0.0057uM
1,1,1-trifluoro-3-octylsulfanylpropan-2-one316358: Inhibition of human recombinant carboxylesterase 2 after 15 minsic500.0058uM
1,1,1-trifluoro-3-hexylsulfanylpropan-2-one48316: In vitro inhibition of carboxylesterase in human liver microsomes.ic500.0069uM
1,1,1-trifluoro-3-octylsulfinylpropan-2-one316358: Inhibition of human recombinant carboxylesterase 2 after 15 minsic500.0074uM
1-(2-chlorophenyl)-2-(3,4-dimethoxyphenyl)ethane-1,2-dione239272: Inhibition constant against human intestinal carboxylesterase 2 (hiCE) using nitrophenyl acetate (o-NPA) as substrateki0.0089uM
ethyl (Z)-4,4,4-trifluoro-2-[(4-fluorophenyl)diazenyl]-3-hydroxybut-2-enoate1762417: Inhibition of human recombinant CES2 expressed in mouse NSO cells using 4-NPA as substrate by spectrophotometric analysisic500.0098uM
N-(2,4-difluorophenyl)-2-[1-(2-oxo-2-pyrrolidin-1-ylethyl)indol-3-yl]sulfanylacetamide2099495: Inhibition of human recombinant CES2 activity assessed as fluorescence of the AP product using Benz-AP as substrateic500.0100uM
(6,7-dimethoxy-1-methyl-3,4-dihydro-1H-isoquinolin-2-yl)-(5,5-dioxo-4H-thieno[3,2-c]thiochromen-2-yl)methanone2099495: Inhibition of human recombinant CES2 activity assessed as fluorescence of the AP product using Benz-AP as substrateic500.0100uM
N-benzyl-4-(4-methylanilino)furo[3,2-c]pyridine-6-carboxamide2099495: Inhibition of human recombinant CES2 activity assessed as fluorescence of the AP product using Benz-AP as substrateic500.0100uM
1-(4-methoxyphenyl)-2-phenylethane-1,2-dione239272: Inhibition constant against human intestinal carboxylesterase 2 (hiCE) using nitrophenyl acetate (o-NPA) as substrateki0.0103uM
ethyl (Z)-2-[(4-bromophenyl)diazenyl]-4,4,4-trifluoro-3-hydroxybut-2-enoate1762417: Inhibition of human recombinant CES2 expressed in mouse NSO cells using 4-NPA as substrate by spectrophotometric analysisic500.0108uM
1,2-bis(2,3,4-trifluorophenyl)ethane-1,2-dione295501: Inhibition of human intestinal carboxylesteraseki0.0136uM
1,2-diphenylethane-1,2-dione239272: Inhibition constant against human intestinal carboxylesterase 2 (hiCE) using nitrophenyl acetate (o-NPA) as substrateki0.0147uM
methyl (Z)-4,4,4-trifluoro-3-hydroxy-2-[(2-nitrophenyl)diazenyl]but-2-enoate1762417: Inhibition of human recombinant CES2 expressed in mouse NSO cells using 4-NPA as substrate by spectrophotometric analysisic500.0169uM
5-(3,4-dimethoxyphenyl)-3-[1-[(3-fluorophenyl)methyl]-5-methyltriazol-4-yl]-1,2,4-oxadiazole2099509: Mixed type of inhibition at human recombinant CES2 activity assessed as fluorescence of the AP product using Benz-AP as substrateki0.0170uM
8,9-dimethyl-3-[(5-methylfuran-2-yl)methyl]-4H-[1,3]oxazino[6,5-b]quinolin-2-one2099495: Inhibition of human recombinant CES2 activity assessed as fluorescence of the AP product using Benz-AP as substrateic500.0180uM
1-(4-chlorophenyl)-2-phenylethane-1,2-dione239272: Inhibition constant against human intestinal carboxylesterase 2 (hiCE) using nitrophenyl acetate (o-NPA) as substrateki0.0182uM
1,2-bis(4-bromophenyl)ethane-1,2-dione239314: Inhibition constant against human intestinal carboxylesterase 2 using 4-MUA (4-methylumbelliferone acetate) as substrateki0.0186uM
4-[[(3S,4aR,6aR,6bS,8aS,11S,12aR,14aR,14bR)-11-ethoxycarbonyl-4,4,6a,6b,8a,11,14b-heptamethyl-1,2,3,4a,5,6,7,8,9,10,12,12a,14,14a-tetradecahydropicen-3-yl]oxy]-4-oxobutanoic acid1285099: Inhibition of CE2 in human liver microsomes using fluorescein diacetate as substrate preincubated for 10 mins followed by substrate addition measured after 30 mins by LC-UV analysisic500.0200uM
1,1,1-trifluorododecan-2-one316358: Inhibition of human recombinant carboxylesterase 2 after 15 minsic500.0200uM
1,1,1-trifluoro-3-octylsulfonylpropan-2-one316358: Inhibition of human recombinant carboxylesterase 2 after 15 minsic500.0210uM
1-[4-(bromomethyl)phenyl]-2-phenylethane-1,2-dione239272: Inhibition constant against human intestinal carboxylesterase 2 (hiCE) using nitrophenyl acetate (o-NPA) as substrateki0.0213uM
1-(4-chlorophenyl)-2-(4-methylphenyl)ethane-1,2-dione239272: Inhibition constant against human intestinal carboxylesterase 2 (hiCE) using nitrophenyl acetate (o-NPA) as substrateki0.0228uM
1,2-bis(3,5-difluorophenyl)ethane-1,2-dione731514: Inhibition of human iCE using o-NPA as substrate by spectrophotometric assayki0.0230uM
ethyl (Z)-4,4,4-trifluoro-3-hydroxy-2-[(3-methylphenyl)diazenyl]but-2-enoate1762417: Inhibition of human recombinant CES2 expressed in mouse NSO cells using 4-NPA as substrate by spectrophotometric analysisic500.0234uM
hexadecane-8,9-dione612131: Inhibition of human intestinal carboxylesterase using o-nitrophenyl acetate as substrate after 5 mins by spectrophotometryki0.0256uM
2-hydroxy-1,2-bis(2,3,4-trifluorophenyl)ethanone295501: Inhibition of human intestinal carboxylesteraseki0.0257uM
1,2-bis(3-fluorophenyl)ethane-1,2-dione295501: Inhibition of human intestinal carboxylesteraseki0.0259uM
1,2-bis(4-chlorophenyl)ethane-1,2-dione239314: Inhibition constant against human intestinal carboxylesterase 2 using 4-MUA (4-methylumbelliferone acetate) as substrateki0.0275uM
1-phenyloctane-1,2-dione612131: Inhibition of human intestinal carboxylesterase using o-nitrophenyl acetate as substrate after 5 mins by spectrophotometryki0.0287uM
1-(4-nitrophenyl)-2-phenylethane-1,2-dione239272: Inhibition constant against human intestinal carboxylesterase 2 (hiCE) using nitrophenyl acetate (o-NPA) as substrateki0.0306uM
1,2-bis(2,3,5-trifluorophenyl)ethane-1,2-dione295501: Inhibition of human intestinal carboxylesteraseki0.0319uM
1-[(4-chlorophenyl)methyl]indole-2,3-dione731514: Inhibition of human iCE using o-NPA as substrate by spectrophotometric assayki0.0320uM
1,1,1,3,3-pentafluorodecan-2-one48316: In vitro inhibition of carboxylesterase in human liver microsomes.ic500.0324uM
1-(4-methylphenyl)-2-phenylethane-1,2-dione239272: Inhibition constant against human intestinal carboxylesterase 2 (hiCE) using nitrophenyl acetate (o-NPA) as substrateki0.0333uM
4-(4-iodophenoxy)naphthalene-1,2-dione1431883: Inhibition of human intestinal CES2 expressed in baculovirus infected sf9 cells using o-nitrophenyl acetate as substrate monitored at 15 secs interval for 5 minski0.0339uM
azepan-1-yl-[2-(1-ethylpyrrolo[2,3-b]pyridin-3-yl)-4-methyl-1,3-thiazol-5-yl]methanone2099509: Mixed type of inhibition at human recombinant CES2 activity assessed as fluorescence of the AP product using Benz-AP as substrateki0.0350uM
8,8-dimethyl-2-propan-2-yl-6,7-dihydro-5H-phenanthrene-3,4-dione731514: Inhibition of human iCE using o-NPA as substrate by spectrophotometric assayki0.0400uM
1-(2,3,5-trifluorophenyl)-2-(2,3,6-trifluorophenyl)ethane-1,2-dione295501: Inhibition of human intestinal carboxylesteraseki0.0407uM
6-[1-(4,6-dimethylpyrimidin-2-yl)piperidin-4-yl]-1-[(3-methoxyphenyl)methyl]-5,6-dihydro-2H-azepin-7-one2099495: Inhibition of human recombinant CES2 activity assessed as fluorescence of the AP product using Benz-AP as substrateic500.0430uM

CTD chemical–gene interactions

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

ChemicalActions (top 5)PubMed papers
Irinotecanincreases abundance, increases chemical synthesis, increases activity, affects response to substance, increases hydrolysis (+4 more)11
Permethrinincreases metabolic processing, affects hydrolysis, increases hydrolysis4
Benzo(a)pyreneincreases expression, increases methylation3
Cisplatinaffects response to substance, affects cotreatment, increases expression, decreases expression3
Cocaineincreases hydrolysis, decreases reaction, increases chemical synthesis, decreases expression3
Heroinincreases hydrolysis, decreases reaction3
Fluorouracilaffects binding, increases reaction, increases expression, affects reaction3
Loperamideincreases response to substance, decreases activity3
Cyclosporineaffects cotreatment, affects expression, decreases expression3
Aflatoxin B1affects expression, decreases expression, increases expression, increases methylation3
bisphenol Adecreases expression, increases expression2
6-O-monoacetylmorphinedecreases reaction, increases chemical synthesis, increases hydrolysis2
Capecitabineincreases response to substance, increases activity, increases hydrolysis2
Acetaminophendecreases expression2
Aspirinaffects hydrolysis, increases hydrolysis2
Doxorubicinaffects expression, increases expression2
Procaineincreases hydrolysis2
Rifampindecreases reaction, increases expression, increases reaction2
GSK-J4decreases expression1
lesinuraddecreases activity1
bisphenol Fincreases expression1
methyl 2-(1-(4-fluorobenzyl)-1H-indazole-3-carboxamido)-3-methylbutanoateincreases metabolic processing1
sanggenon Ddecreases activity1
bis(4-nitrophenyl)phosphatedecreases activity1
testosterone enanthateaffects expression1
methylmercuric chloridedecreases expression1
lasiocarpinedecreases expression1
oxybutyninincreases hydrolysis1
triphenyl phosphateaffects expression1
alpha-pineneaffects cotreatment, increases oxidation, increases abundance1

ChEMBL screening assays

114 unique, capped per target: 58 binding, 56 admet

Representative assays (with source publication via chembl_document):

Assay IDTypeDescriptionSource paper
CHEMBL1040871BindingInhibition of human CES2-mediated pNPA substrate turnoverIsosorbide-2-benzyl carbamate-5-salicylate, a peripheral anionic site binding subnanomolar selective butyrylcholinesterase inhibitor. — J Med Chem
CHEMBL1781735ADMETActivity at carboxylesterase in human HT-1080 cells assessed as accumulation of resorufin in nucleus at 50 uM after 120 mins by phase contrast microscopic analysisDesign and synthesis of an ER-specific fluorescent probe based on carboxylesterase activity with quinone methide cleavage process. — Bioorg Med Chem Lett

Cellosaurus cell lines

2 cell lines: 2 cancer cell line

First 10 cell lines (id-ordered, not curated):

CellosaurusNameCategorySex
CVCL_E1TMHAP1 CES2 (-) 1Cancer cell lineMale
CVCL_E1TNHAP1 CES2 (-) 2Cancer cell lineMale

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_promotergenccgenerifgogoparentgtopdbgtopdb_interactiongwasgwas_studyhgnchpointactinterprointogenjasparmeshmimmirdbmondomsigdborphanetorthologparalogpatent_compoundpdbpfampharmgkb_clinicalpharmgkb_genepharmgkb_guidelinepharmgkb_variantpubchempubchem_activitypubchem_assaypubmedreactomereactomeparentrefseqrhearnacentralscxa_expressionscxa_gene_experimentsignorspliceaistring_interactiontranscriptufeatureuniprot