SOAT2
gene geneOn this page
Also known as ACAT2
Summary
SOAT2 (sterol O-acyltransferase 2, HGNC:11178) is a protein-coding gene on chromosome 12q13.13, encoding Sterol O-acyltransferase 2 (O75908). Catalyzes the formation of fatty acid-cholesterol esters, which are less soluble in membranes than cholesterol.
Summary:This gene is a member of a small family of acyl coenzyme A:cholesterol acyltransferases. The gene encodes a membrane-bound enzyme localized in the endoplasmic reticulum that produces intracellular cholesterol esters from long-chain fatty acyl CoA and cholesterol. The cholesterol esters are then stored as cytoplasmic lipid droplets inside the cell. The enzyme is implicated in cholesterol absorption in the intestine and in the assembly and secretion of apolipoprotein B-containing lipoproteins such as very low density lipoprotein (VLDL). Several alternatively spliced transcript variants of this gene have been described, but their full-length nature is not known.
Source: NCBI Gene 8435 — RefSeq curated summary.
At a glance
- GWAS associations: 2
- Clinical variants (ClinVar): 94 total
- Druggable target: yes — 4 molecules with ChEMBL bioactivity
- MANE Select transcript:
NM_003578
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:11178 |
| Approved symbol | SOAT2 |
| Name | sterol O-acyltransferase 2 |
| Location | 12q13.13 |
| Locus type | gene with protein product |
| Status | Approved |
| Aliases | ACAT2 |
| Ensembl gene | ENSG00000167780 |
| Ensembl biotype | protein_coding |
| OMIM | 601311 |
| Entrez | 8435 |
Gene structure
Transcript identifiers
Ensembl transcripts: 10 — 9 protein_coding, 1 nonsense_mediated_decay
ENST00000301466, ENST00000542365, ENST00000551896, ENST00000869109, ENST00000869110, ENST00000869111, ENST00000869112, ENST00000869113, ENST00000869114, ENST00000869115
RefSeq mRNA: 1 — MANE Select: NM_003578
NM_003578
CCDS: CCDS8847
Canonical transcript exons
ENST00000301466 — 15 exons
| Exon | Start | End |
|---|---|---|
| ENSE00001116928 | 53105561 | 53105620 |
| ENSE00001116936 | 53118350 | 53118434 |
| ENSE00001116938 | 53105107 | 53105243 |
| ENSE00001116941 | 53105907 | 53106014 |
| ENSE00001116942 | 53115390 | 53115654 |
| ENSE00001116944 | 53104151 | 53104206 |
| ENSE00001116946 | 53116097 | 53116166 |
| ENSE00001116951 | 53118890 | 53118935 |
| ENSE00001592033 | 53124073 | 53124535 |
| ENSE00003468381 | 53123081 | 53123216 |
| ENSE00003471668 | 53123728 | 53123873 |
| ENSE00003606078 | 53119124 | 53119253 |
| ENSE00003639233 | 53121303 | 53121401 |
| ENSE00003658052 | 53120786 | 53120883 |
| ENSE00003848576 | 53103486 | 53103659 |
Expression profiles
Bgee: expression breadth ubiquitous, 124 present calls, max score 88.13.
FANTOM5 (CAGE): breadth tissue_specific, TPM avg 0.4956 / max 100.3321, expressed in 100 samples.
FANTOM5 promoters (3 alternative TSS)
| Promoter ID | TPM avg | Samples expressed |
|---|---|---|
| 125708 | 0.4230 | 82 |
| 125706 | 0.0383 | 21 |
| 125707 | 0.0343 | 21 |
Top tissues by expression
276 total, by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| jejunal mucosa | UBERON:0000399 | 88.13 | gold quality |
| male germ line stem cell (sensu Vertebrata) in testis | CL:0000089 ∩ UBERON:0000473 | 87.51 | gold quality |
| primordial germ cell in gonad | CL:0000670 ∩ UBERON:0000991 | 84.21 | gold quality |
| duodenum | UBERON:0002114 | 80.36 | gold quality |
| spleen | UBERON:0002106 | 74.32 | gold quality |
| right lobe of liver | UBERON:0001114 | 70.62 | gold quality |
| small intestine | UBERON:0002108 | 69.21 | gold quality |
| small intestine Peyer’s patch | UBERON:0003454 | 68.31 | gold quality |
| jejunum | UBERON:0002115 | 66.78 | gold quality |
| ileal mucosa | UBERON:0000331 | 65.45 | silver quality |
| mucosa of stomach | UBERON:0001199 | 64.33 | gold quality |
| tibial nerve | UBERON:0001323 | 63.49 | gold quality |
| liver | UBERON:0002107 | 63.40 | gold quality |
| thoracic aorta | UBERON:0001515 | 62.96 | gold quality |
| ascending aorta | UBERON:0001496 | 62.85 | gold quality |
| descending thoracic aorta | UBERON:0002345 | 62.53 | gold quality |
| aorta | UBERON:0000947 | 62.42 | gold quality |
| popliteal artery | UBERON:0002250 | 62.14 | gold quality |
| tibial artery | UBERON:0007610 | 62.08 | gold quality |
| trabecular bone tissue | UBERON:0002483 | 61.48 | gold quality |
| granulocyte | CL:0000094 | 60.26 | gold quality |
| endocervix | UBERON:0000458 | 60.24 | gold quality |
| decidua | UBERON:0002450 | 59.05 | gold quality |
| left coronary artery | UBERON:0001626 | 58.82 | gold quality |
| secondary oocyte | CL:0000655 | 58.15 | gold quality |
| right coronary artery | UBERON:0001625 | 57.97 | gold quality |
| coronary artery | UBERON:0001621 | 57.74 | gold quality |
| gingival epithelium | UBERON:0001949 | 57.24 | gold quality |
| left uterine tube | UBERON:0001303 | 56.67 | gold quality |
| skin of leg | UBERON:0001511 | 56.47 | gold quality |
Single-cell (SCXA)
Detected in 1 experiment(s), a significant marker in 0.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-ANND-3 | no | 1.55 |
Regulation
Is transcription factor: no
Upstream regulators (CollecTRI, top): HNF1B, HNF4A
miRNA regulators (miRDB)
16 targeting SOAT2, top 30 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific):
| miRNA | Max score | Avg score | miRNA target_count |
|---|---|---|---|
| HSA-MIR-4533 | 100.00 | 69.48 | 2758 |
| HSA-MIR-6721-5P | 99.93 | 68.92 | 2981 |
| HSA-MIR-137-3P | 99.87 | 74.74 | 2401 |
| HSA-MIR-6857-5P | 99.87 | 65.32 | 985 |
| HSA-MIR-4999-5P | 99.35 | 69.15 | 926 |
| HSA-MIR-7160-5P | 99.11 | 67.17 | 2207 |
| HSA-MIR-6760-5P | 98.87 | 66.73 | 1515 |
| HSA-MIR-502-5P | 98.77 | 66.51 | 906 |
| HSA-MIR-6894-5P | 98.70 | 63.78 | 809 |
| HSA-MIR-4726-3P | 98.49 | 63.89 | 1385 |
| HSA-MIR-6780A-3P | 98.42 | 67.49 | 1518 |
| HSA-MIR-581 | 98.39 | 67.42 | 835 |
| HSA-MIR-3166 | 98.24 | 66.63 | 1223 |
| HSA-MIR-6511B-5P | 97.98 | 65.64 | 823 |
| HSA-MIR-6811-5P | 97.98 | 64.96 | 848 |
| HSA-MIR-4264 | 96.35 | 64.76 | 1480 |
Literature-anchored findings (GeneRIF, showing 28)
- We found a new single-nucleotide polymorphism (SNP; a point mutation in intron 1, IVS1 -8 G–>C) in the ACAT-2 gene. Our data suggest that the ACAT-2 gene may not affect lipid levels in humans. (PMID:12621162)
- Fully differentiated macrophages express ACAT2 in addition to ACAT1 under various pathologic conditions. (PMID:14615411)
- ACAT-1 transcripts predominate in human liver and ACAT-2 transcripts predominate in human duodenum and support the notion that ACAT-2 has an important regulatory role in liver and intestine. (PMID:14729857)
- increasing DGAT1, ACAT1, or ACAT2 expression stimulates the assembly and secretion of VLDL from liver cells (PMID:15308631)
- ACAT2 provided the major cholesterol-esterifying activity in 3 of 4 human liver samples. (PMID:15451793)
- transcription factors hepatic nuclear factor 1 (HNF1)alpha and beta play an important part in the regulation of the ACAT2 promoter (PMID:15961790)
- The structural features of various sterols as substrates and/or activators of ACAT1 and ACAT2 in vitro are reported. (PMID:15992359)
- Serum-induced depletion of cellular cholesterol available for esterification by ACAT was a strong, independent predictor of major adverse cardiovascular events and death. (PMID:16230498)
- Elevated ACAT2 expression may serve as a new biomarker for certain form(s) of hepatocellular carcinoma. (PMID:16274362)
- Alternative splicing produces two human ACAT2 mRNA variants that encode the novel ACAT2 isoenzymes. Our findings might help to understand the regulation of the ACAT2 gene expression under certain physiological and pathological conditions. (PMID:16331323)
- histidine residues located at the active site are very crucial both for the catalytic activity of the enzyme and for distinguishing ACAT1 from ACAT2 with respect to enzyme catalysis and substrate specificity (PMID:16647063)
- We resequenced 4 candidate genes for HDL regulation and identified several functional nonsynonymous mutations including 4 in lecithin:cholesterol acyltransferase (LCAT), leaving 88% (110/124) of HDL deficient subjects without a genetic diagnosis. (PMID:17303779)
- human ACAT2 is transcriptionally regulated by cholesterol. (PMID:17950700)
- ACAT2 expression was induced upon R1881 (androgen agonist) treatment in prostate cancer cells (PMID:18000807)
- ACAT-2 expression was negative in clear cell type renal cell carcinoma and normal kidney. (PMID:18269457)
- Describe a gender-related difference in hepatic ACAT2 activity in normolipidemic non-obese Chinese patients suggesting a possible role for ACAT2 in the regulation of cholesterol metabolism in humans. (PMID:19467657)
- HNF4alpha positively regulates ACAT2 gene expression at mRNA level. Overexpression of HNF4alpha increased ACAT2 expression, whereas knockdown of HNF4alpha decreased ACAT2 expression. (PMID:22155889)
- CDX2, a known positive regulator of hepatocyte differentiation, was regulated by miR-181d and directly activated SOAT2 gene expression. (PMID:24103759)
- TG-interacting factor 1 (Tgif1) is an important repressor of SOAT2 gene expression. (PMID:24478032)
- results show that the enzymatic activity of mutant Glu(14)Gly is approximately two times higher than wildtype, and that this increase is primarily due to the increased expression and/or stability of the mutant ACAT2 protein (PMID:25917363)
- Low ACAT2 expression is associated with clear cell renal cell carcinoma. (PMID:26715271)
- data demonstrate that the ACAT2 expression of human leukocytes is responsible for the excretion of lipoproteins containing cholesteryl/steryl esters (CE/SE), and suggest that the excretion of lipoproteins containing the ACAT2-catalyzed CS/SE may avoid cytotoxicity (PMID:27688150)
- Lipid-induced stabilization of ACAT2 ameliorates lipotoxicity from excessive cholesterol and fatty acid. Cysteine ubiquitylation of ACAT2 constitutes an important mechanism for sensing lipid-overload-induced ROS and fine-tuning lipid homeostasis. (PMID:28604676)
- Single nucleotide polymorphisms Rs28765985 of ACAT-2 (SOAT2) gene are associated with increased susceptibility to coronary artery disease in Uygur population in Xinjiang, China. (PMID:30696703)
- Whole-exome sequencing and genome-wide association studies identify novel sarcopenia risk genes in Han Chinese. (PMID:32478482)
- Sterol O-acyltransferase 2 chaperoned by apolipoprotein J facilitates hepatic lipid accumulation following viral and nutrient stresses. (PMID:33980978)
- Identification of the prognostic value of Th1/Th2 ratio and a novel prognostic signature in basal-like breast cancer. (PMID:36694223)
- ACAT2 may be a novel predictive biomarker and therapeutic target in lung adenocarcinoma. (PMID:38213102)
Cross-species orthologs
5 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| danio_rerio | soat2 | ENSDARG00000059824 |
| mus_musculus | Soat2 | ENSMUSG00000023045 |
| rattus_norvegicus | Soat2 | ENSRNOG00000053769 |
| drosophila_melanogaster | CG8112 | FBGN0037612 |
| caenorhabditis_elegans | WBGENE00007174 |
Paralogs (2): SOAT1 (ENSG00000057252), DGAT1 (ENSG00000185000)
Protein
Protein identifiers
Sterol O-acyltransferase 2 — O75908 (reviewed: O75908)
Alternative names: Acyl-coenzyme A:cholesterol acyltransferase 2, Cholesterol acyltransferase 2
All UniProt accessions (2): O75908, F8VPE9
UniProt curated annotations — full annotation on UniProt →
Function. Catalyzes the formation of fatty acid-cholesterol esters, which are less soluble in membranes than cholesterol. Plays a role in lipoprotein assembly and dietary cholesterol absorption. Utilizes oleoyl-CoA ((9Z)-octadecenoyl-CoA) and linolenoyl-CoA ((9Z,12Z,15Z)-octadecatrienoyl-CoA) as substrates. May provide cholesteryl esters for lipoprotein secretion from hepatocytes and intestinal mucosa. Has lower enzymatic activity compared to isoform 1. Has lower enzymatic activity compared to isoform 1.
Subunit / interactions. May form homo- or heterodimers. Interacts with INSIG1; the interaction is direct and promotes association with AMFR/gp78.
Subcellular location. Endoplasmic reticulum membrane.
Tissue specificity. Expression seems confined in hepatocytes and enterocytes.
Post-translational modifications. Polyubiquitinated by AMFR/gp78 at Cys-277, leading to its degradation when the lipid levels are low. Association with AMFR/gp78 is mediated via interaction with INSIG1. High concentration of cholesterol and fatty acid results in Cys-277 oxidation, preventing ubiquitination at the same site, resulting in protein stabilization. Oxidized at Cys-277: high concentration of cholesterol and fatty acid induce reactive oxygen species, which oxidizes Cys-277, preventing ubiquitination at the same site, and resulting in protein stabilization.
Domain organisation. Each protomer consists of 9 transmembrane segments, which enclose a cytosolic tunnel and a transmembrane tunnel that converge at the predicted catalytic site: acyl-CoA enters the active site through the cytosolic tunnel, whereas cholesterol enters from the side through the transmembrane tunnel.
Similarity. Belongs to the membrane-bound acyltransferase family. Sterol o-acyltransferase subfamily.
Isoforms (4)
| UniProt ID | Names | Canonical? |
|---|---|---|
| O75908-1 | 1, ACAD2a | yes |
| O75908-2 | 2, ACAD2b | |
| O75908-3 | 3, ACAD2c | |
| O75908-4 | 4 |
RefSeq proteins (1): NP_003569* (*=MANE)
Domains & families (InterPro)
| ID | Name | Type |
|---|---|---|
| IPR004299 | MBOAT_fam | Family |
| IPR014371 | Oat_ACAT_DAG_ARE | Family |
| IPR030687 | Sterol_acyltranf_meta | Family |
Pfam: PF03062
Enzyme classification (BRENDA):
- EC 2.3.1.26 — sterol O-acyltransferase (BRENDA: 24 organisms, 85 substrates, 472 inhibitors, 32 Km, 0 kcat entries)
Substrate kinetics (BRENDA)
8 substrates with measured Km, best-characterized 8. Km ranges are aggregated across organisms/conditions.
| Substrate | Km (mM) | Measurements |
|---|---|---|
| OLEOYL-COA | 0.0013–0.069 | 12 |
| CIS-9-OCTADECENOYL-COA | — | 6 |
| CHOLESTEROL | 0.0016–0.06 | 2 |
| ELAIDOYL-COA | 0.0022 | 1 |
| LINOLEOYL-COA | 0.0028 | 1 |
| PALMITOYL-COA | 0.038 | 1 |
| PREGNENOLONE | 0.0012 | 1 |
| STEAROYL-COA | 0.0064 | 1 |
Catalyzed reactions (Rhea), 6 shown:
- an acyl-CoA + cholesterol = a cholesterol ester + CoA (RHEA:17729)
- cholesterol + (9Z)-octadecenoyl-CoA = cholesteryl (9Z-octadecenoate) + CoA (RHEA:41436)
- (5Z,8Z,11Z,14Z)-eicosatetraenoyl-CoA + cholesterol = cholesteryl (5Z,8Z,11Z,14Z)-eicosatetraenoate + CoA (RHEA:42816)
- (5Z,8Z,11Z,14Z,17Z)-eicosapentaenoyl-CoA + cholesterol = (5Z,8Z,11Z,14Z,17Z-eicosapentaenoyl)-cholesterol + CoA (RHEA:46612)
- (9Z,12Z,15Z)-octadecatrienoyl-CoA + cholesterol = (9Z,12Z,15Z-octadecatrienoyl)-cholesterol + CoA (RHEA:46620)
- a sterol + a long-chain fatty acyl-CoA = a long-chain 3-hydroxysterol ester + CoA (RHEA:59816)
UniProt features (55 total): mutagenesis site 13, topological domain 10, transmembrane region 9, binding site 7, splice variant 5, region of interest 2, sequence variant 2, chain 1, short sequence motif 1, compositionally biased region 1, active site 1, modified residue 1, cross-link 1, sequence conflict 1
Structure
Experimental structures (PDB)
2 structures.
| PDB | Method | Resolution (Å) |
|---|---|---|
| 7N6Q | ELECTRON MICROSCOPY | 3.87 |
| 7N6R | ELECTRON MICROSCOPY | 3.93 |
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-O75908-F1 | 82.59 | 0.49 |
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 (1): 434
Ligand- & substrate-binding residues (7): 119; 389; 392; 395; 399; 407; 430
Post-translational modifications (2): 277, 277
Mutagenesis-validated functional residues (13):
| Position | Phenotype |
|---|---|
| 49 | in k-null mutant; does not affect ubiquitination and sterol-regulated stabilization; when associated with r-80, r-100, r |
| 80 | in k-null mutant; does not affect ubiquitination and sterol-regulated stabilization; when associated with r-49, r-100, r |
| 100 | in k-null mutant; does not affect ubiquitination and sterol-regulated stabilization; when associated with r-49, r-80, r- |
| 102 | in k-null mutant; does not affect ubiquitination and sterol-regulated stabilization; when associated with r-49, r-80, r- |
| 108 | in k-null mutant; does not affect ubiquitination and sterol-regulated stabilization; when associated with r-49, r-80, r- |
| 242 | in k-null mutant; does not affect ubiquitination and sterol-regulated stabilization; when associated with r-49, r-80, r- |
| 254 | does not affect ubiquitination and sterol-regulated stabilization; when associated with r-279. |
| 267–270 | does not affect ubiquitination and sterol-regulated stabilization. |
| 277 | abolished ubiquitination and sterol-regulated stabilization. |
| 279 | does not affect ubiquitination and sterol-regulated stabilization; when associated with r-54. |
| 299 | in k-null mutant; does not affect ubiquitination and sterol-regulated stabilization; when associated with r-49, r-80, r- |
| 360 | abolished cholesterol o-acyltransferase activity. |
| 399 | abolished cholesterol o-acyltransferase activity. |
Function
Pathways and Gene Ontology
Reactome pathways
4 pathways
| ID | Pathway |
|---|---|
| R-HSA-8964038 | LDL clearance |
| R-HSA-174824 | Plasma lipoprotein assembly, remodeling, and clearance |
| R-HSA-382551 | Transport of small molecules |
| R-HSA-8964043 | Plasma lipoprotein clearance |
MSigDB gene sets: 419 (showing top):
GSE45365_CTRL_VS_MCMV_INFECTION_NK_CELL_UP, GOBP_DIGESTION, HORIUCHI_WTAP_TARGETS_DN, GOBP_PHOSPHOLIPID_METABOLIC_PROCESS, GOBP_STEROL_HOMEOSTASIS, STARK_PREFRONTAL_CORTEX_22Q11_DELETION_DN, YANG_BREAST_CANCER_ESR1_LASER_DN, ACEVEDO_NORMAL_TISSUE_ADJACENT_TO_LIVER_TUMOR_DN, GOBP_ORGANOPHOSPHATE_METABOLIC_PROCESS, GOBP_POSITIVE_REGULATION_OF_DIGESTIVE_SYSTEM_PROCESS, GOBP_PROTEIN_LIPID_COMPLEX_ASSEMBLY, GOBP_MONOCARBOXYLIC_ACID_METABOLIC_PROCESS, GOBP_ORGANOPHOSPHATE_BIOSYNTHETIC_PROCESS, MORF_RAD51L3, GOBP_LOW_DENSITY_LIPOPROTEIN_PARTICLE_CLEARANCE
GO Biological Process (11): cholesterol metabolic process (GO:0008203), macrophage derived foam cell differentiation (GO:0010742), cholesterol storage (GO:0010878), intestinal cholesterol absorption (GO:0030299), cholesterol efflux (GO:0033344), very-low-density lipoprotein particle assembly (GO:0034379), low-density lipoprotein particle clearance (GO:0034383), cholesterol homeostasis (GO:0042632), positive regulation of intestinal cholesterol absorption (GO:0045797), lipid metabolic process (GO:0006629), steroid metabolic process (GO:0008202)
GO Molecular Function (8): fatty-acyl-CoA binding (GO:0000062), sterol O-acyltransferase activity (GO:0004772), cholesterol binding (GO:0015485), acyltransferase activity (GO:0016746), cholesterol O-acyltransferase activity (GO:0034736), protein binding (GO:0005515), obsolete O-acyltransferase activity (GO:0008374), transferase activity (GO:0016740)
GO Cellular Component (4): endoplasmic reticulum (GO:0005783), endoplasmic reticulum membrane (GO:0005789), brush border (GO:0005903), membrane (GO:0016020)
Reactome top-level categories
Rollup of top-3 pathways:
| Category | Pathways |
|---|---|
| Plasma lipoprotein clearance | 1 |
| Transport of small molecules | 1 |
| Plasma lipoprotein assembly, remodeling, and clearance | 1 |
GO top-level categories
Rollup of top GO terms by namespace:
| Category | Terms |
|---|---|
| sterol metabolic process | 1 |
| secondary alcohol metabolic process | 1 |
| foam cell differentiation | 1 |
| lipid storage | 1 |
| lipid digestion | 1 |
| intestinal lipid absorption | 1 |
| cholesterol transport | 1 |
| plasma lipoprotein particle assembly | 1 |
| plasma lipoprotein particle clearance | 1 |
| low-density lipoprotein particle disassembly | 1 |
| sterol homeostasis | 1 |
| intestinal cholesterol absorption | 1 |
| regulation of intestinal cholesterol absorption | 1 |
| positive regulation of intestinal lipid absorption | 1 |
| primary metabolic process | 1 |
| lipid metabolic process | 1 |
| acyl-CoA binding | 1 |
| fatty acid derivative binding | 1 |
| acyltransferase activity, transferring groups other than amino-acyl groups | 1 |
| sterol binding | 1 |
| alcohol binding | 1 |
| transferase activity | 1 |
| sterol O-acyltransferase activity | 1 |
| binding | 1 |
| catalytic activity | 1 |
| cytoplasm | 1 |
| endomembrane system | 1 |
| intracellular membrane-bounded organelle | 1 |
| organelle membrane | 1 |
| nuclear outer membrane-endoplasmic reticulum membrane network | 1 |
| endoplasmic reticulum subcompartment | 1 |
| microvillus | 1 |
| apical part of cell | 1 |
| cluster of actin-based cell projections | 1 |
| cellular anatomical structure | 1 |
Protein interactions and networks
STRING
1204 interactions, top by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| SOAT2 | VPS52 | Q8N1B4 | 856 |
| SOAT2 | IGFBP6 | P24592 | 837 |
| SOAT2 | KRT2 | P35908 | 736 |
| SOAT2 | APOB | P04114 | 707 |
| SOAT2 | DGAT2 | Q96PD7 | 705 |
| SOAT2 | HMGCR | P04035 | 664 |
| SOAT2 | NPC1L1 | Q9UHC9 | 628 |
| SOAT2 | RARG | P13631 | 615 |
| SOAT2 | LCAT | P04180 | 608 |
| SOAT2 | ABCG5 | Q9H222 | 599 |
| SOAT2 | ITGB7 | P26010 | 554 |
| SOAT2 | ABCG8 | Q9H221 | 547 |
| SOAT2 | SREBF2 | Q12772 | 519 |
| SOAT2 | APOE | P02649 | 517 |
| SOAT2 | MTTP | P55157 | 509 |
IntAct
10 interactions, top by confidence:
| A | B | Type | Score |
|---|---|---|---|
| SOAT2 | TMBIM6 | psi-mi:“MI:0915”(physical association) | 0.560 |
| SOAT2 | AKT1 | psi-mi:“MI:0915”(physical association) | 0.370 |
| KSR1 | FBLL1 | psi-mi:“MI:0914”(association) | 0.350 |
| RBM15 | ILVBL | psi-mi:“MI:2364”(proximity) | 0.270 |
| SF3B4 | MED19 | psi-mi:“MI:2364”(proximity) | 0.270 |
| YWHAG | RPSA2 | psi-mi:“MI:2364”(proximity) | 0.270 |
| DDX6 | RPSA2 | psi-mi:“MI:2364”(proximity) | 0.270 |
| TMBIM6 | SOAT2 | psi-mi:“MI:0915”(physical association) | 0.000 |
BioGRID (8): AMFR (Affinity Capture-MS), AMFR (Affinity Capture-Western), INSIG1 (Affinity Capture-Western), SOAT2 (Synthetic Lethality), SOAT2 (Two-hybrid), SOAT2 (Affinity Capture-Western), SOAT2 (Affinity Capture-MS), SOAT2 (Affinity Capture-Luminescence)
ESM2 similar proteins: A0A8C2M425, A1L1J9, B0BNG2, O60725, O75908, O77759, O88269, O88908, O95255, Q0P4J9, Q290J8, Q3T1L5, Q3TAE8, Q3UV71, Q499P8, Q49LS7, Q4R4E1, Q4VV71, Q5F380, Q5KR61, Q5R8F6, Q5RAH7, Q5RKL5, Q6AZ83, Q6NVG1, Q7SXZ1, Q7T310, Q7TPN3, Q7TQM4, Q86VD9, Q8AVI9, Q8BTP0, Q8C0T0, Q8C3X8, Q8CI59, Q8IUR5, Q8K2A8, Q8L638, Q8R1J1, Q8R4P9
Diamond homologs: A0A0P0WY03, A0A161IUT7, I1MSF2, K7LC65, O70536, O75907, O75908, O77759, O77760, O77761, O88908, P25628, P35610, P53629, P84285, Q55BH9, Q5GKZ7, Q5I396, Q60457, Q61263, Q7TQM4, Q876L2, Q876L3, Q8MK44, Q9ERM3, Q9GMF1, Q9SLD2, Q9Z2A7, Q9UU82, Q10269
SIGNOR signaling
0 interactions.
Disease & clinical
Clinical variants and AI predictions
ClinVar
94 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 0 |
| Likely pathogenic | 0 |
| Uncertain significance | 77 |
| Likely benign | 10 |
| Benign | 3 |
Top pathogenic / likely-pathogenic (0)
SpliceAI
3306 predictions. Top by Δscore:
| Variant | Effect | Δscore |
|---|---|---|
| 12:53105106:GGCT:G | acceptor_gain | 1.0000 |
| 12:53105240:GCAG:G | donor_gain | 1.0000 |
| 12:53105242:AGG:A | donor_loss | 1.0000 |
| 12:53105244:GT:G | donor_loss | 1.0000 |
| 12:53105245:T:A | donor_loss | 1.0000 |
| 12:53105621:G:GG | donor_gain | 1.0000 |
| 12:53105901:CTCTA:C | acceptor_loss | 1.0000 |
| 12:53105903:CTAGT:C | acceptor_loss | 1.0000 |
| 12:53105904:TAGT:T | acceptor_loss | 1.0000 |
| 12:53105904:TAGTG:T | acceptor_gain | 1.0000 |
| 12:53105905:A:AG | acceptor_gain | 1.0000 |
| 12:53105905:AGT:A | acceptor_gain | 1.0000 |
| 12:53105905:AGTGA:A | acceptor_gain | 1.0000 |
| 12:53105906:G:GG | acceptor_gain | 1.0000 |
| 12:53105906:GT:G | acceptor_gain | 1.0000 |
| 12:53105906:GTG:G | acceptor_gain | 1.0000 |
| 12:53105906:GTGA:G | acceptor_gain | 1.0000 |
| 12:53105906:GTGAG:G | acceptor_gain | 1.0000 |
| 12:53106010:GGCAG:G | donor_gain | 1.0000 |
| 12:53106011:GCAG:G | donor_gain | 1.0000 |
| 12:53106011:GCAGG:G | donor_gain | 1.0000 |
| 12:53106012:C:T | donor_gain | 1.0000 |
| 12:53106014:GGTA:G | donor_loss | 1.0000 |
| 12:53106015:GT:G | donor_loss | 1.0000 |
| 12:53106016:T:G | donor_loss | 1.0000 |
| 12:53118346:CCA:C | acceptor_loss | 1.0000 |
| 12:53118349:GGT:G | acceptor_gain | 1.0000 |
| 12:53118349:GGTGA:G | acceptor_gain | 1.0000 |
| 12:53118433:AGGTA:A | donor_loss | 1.0000 |
| 12:53118436:T:A | donor_loss | 1.0000 |
AlphaMissense
3372 scored. Top likely-pathogenic:
| Variant | Protein change | am_pathogenicity |
|---|---|---|
| 12:53121309:T:A | W382R | 0.999 |
| 12:53121309:T:C | W382R | 0.999 |
| 12:53121311:G:C | W382C | 0.998 |
| 12:53121311:G:T | W382C | 0.998 |
| 12:53121306:T:A | W381R | 0.997 |
| 12:53121306:T:C | W381R | 0.997 |
| 12:53121350:C:A | N395K | 0.997 |
| 12:53121350:C:G | N395K | 0.997 |
| 12:53120875:T:C | F377L | 0.996 |
| 12:53120877:C:A | F377L | 0.996 |
| 12:53120877:C:G | F377L | 0.996 |
| 12:53120860:T:C | F372L | 0.995 |
| 12:53120862:T:A | F372L | 0.995 |
| 12:53120862:T:G | F372L | 0.995 |
| 12:53120876:T:C | F377S | 0.995 |
| 12:53121345:T:A | W394R | 0.995 |
| 12:53121345:T:C | W394R | 0.995 |
| 12:53123787:T:A | W478R | 0.994 |
| 12:53123787:T:C | W478R | 0.994 |
| 12:53118391:T:C | F274L | 0.993 |
| 12:53118393:C:A | F274L | 0.993 |
| 12:53118393:C:G | F274L | 0.993 |
| 12:53120876:T:G | F377C | 0.992 |
| 12:53121310:G:C | W382S | 0.992 |
| 12:53121340:G:C | R392P | 0.992 |
| 12:53123823:A:C | S490R | 0.992 |
| 12:53123825:C:A | S490R | 0.992 |
| 12:53123825:C:G | S490R | 0.992 |
| 12:53105595:T:C | F104L | 0.991 |
| 12:53105597:C:A | F104L | 0.991 |
dbSNP variants (sampled 300 via entrez): RS1000013201 (12:53115078 A>G), RS1000209086 (12:53125019 G>A), RS1000830729 (12:53122853 C>T), RS1000836743 (12:53108182 T>A), RS1000893867 (12:53108560 T>C), RS1000948582 (12:53102506 C>T), RS1001117517 (12:53122659 A>C), RS1001216616 (12:53123412 T>A), RS1001229015 (12:53117458 A>G), RS1001301610 (12:53122247 C>A,T), RS1001400859 (12:53102897 C>T), RS1001456807 (12:53111367 A>C,G), RS1001522283 (12:53111358 C>T), RS1001573169 (12:53111720 C>A,G,T), RS1001635585 (12:53104821 G>A)
Disease associations
OMIM: gene MIM:601311 | disease phenotypes:
GenCC curated gene-disease
Mondo (0):
Orphanet (0):
HPO phenotypes
0 total (0 of 0 shown, HPO-id order):
GWAS associations
2 associations (top):
| Study | Trait | p-value |
|---|---|---|
| GCST009144_5 | Disease progression in age-related macular degeneration (adjusted for baseline) | 7.000000e-06 |
| GCST90000025_968 | Appendicular lean mass | 1.000000e-16 |
EFO canonical traits (2, from GWAS)
| EFO ID | Trait name |
|---|---|
| EFO:0008336 | disease progression measurement |
| EFO:0004980 | appendicular lean mass |
Drugs & pharmacology
Drug and pharmacology data
Is drug target: yes
ChEMBL targets (1): CHEMBL4465 (SINGLE PROTEIN)
Molecules with ChEMBL bioactivity
4 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 10,763 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).
| Molecule | Name | Phase | Patents |
|---|---|---|---|
| CHEMBL101309 | AVASIMIBE | 2 | 10,153 |
| CHEMBL1908306 | EFLUCIMIBE | 2 | 272 |
| CHEMBL46423 | NEVANIMIBE | 2 | 78 |
| CHEMBL478858 | PACTIMIBE | 2 | 260 |
PharmGKB: 1 entry (VIP=true, CPIC=false)
Binding affinities (BindingDB)
24 measured of 24 human assays (24 total across all organisms); most potent 24 below. Values come from heterogeneous assays and are not directly comparable.
| Ligand | Measure | Value | Patent |
|---|---|---|---|
| [4-[2-benzyl-5-[2,6-di(propan-2-yl)anilino]-3,5-dioxopentyl]phenyl] 2-(2-oxoazepan-1-yl)acetate | IC50 | 3.2 nM | US-9149492: Method for selectively inhibiting ACAT1 in the treatment of alzheimer’s disease |
| [4-[2-benzyl-5-[2,6-di(propan-2-yl)anilino]-3,5-dioxopentyl]phenyl] 7-(2-oxoazepan-1-yl)heptanoate | IC50 | 3.6 nM | US-9149492: Method for selectively inhibiting ACAT1 in the treatment of alzheimer’s disease |
| 4-benzyl-N-[2,6-di(propan-2-yl)phenyl]-3-oxo-5-phenylpentanamide | IC50 | 4.2 nM | US-9149492: Method for selectively inhibiting ACAT1 in the treatment of alzheimer’s disease |
| 4-benzyl-N-[2,6-di(propan-2-yl)phenyl]-5-(4-hydroxyphenyl)-3-oxopentanamide | IC50 | 10.3 nM | US-9149492: Method for selectively inhibiting ACAT1 in the treatment of alzheimer’s disease |
| (2S)-2-dodecylsulfanyl-N-(4-hydroxy-2,3,5-trimethylphenyl)-2-phenylacetamide | IC50 | 39 nM | US-9149492: Method for selectively inhibiting ACAT1 in the treatment of alzheimer’s disease |
| [(2R)-2-[(5aR,6R,8R,9aR,10S)-6,10-dihydroxy-5a-methyl-1-oxo-3-pyridin-3-yl-6,7,8,9,9a,10-hexahydropyrano[4,3-b]chromen-8-yl]-2-hydroxypropyl] acetate | IC50 | 69 nM | US-10278962: Tricyclic analogues, preparation method and uses thereof |
| [(2R)-2-[(5aR,6R,8R,9aR,10R)-6,10-dihydroxy-5a-methyl-1-oxo-3-pyridin-3-yl-6,7,8,9,9a,10-hexahydropyrano[4,3-b]chromen-8-yl]-2-hydroxypropyl] acetate | IC50 | 81 nM | US-10278962: Tricyclic analogues, preparation method and uses thereof |
| (5,9-diacetyloxy-18-hydroxy-2,6,10-trimethyl-16-oxo-14-pyridin-3-yl-11,15-dioxatetracyclo[8.8.0.02,7.012,17]octadeca-12(17),13-dien-6-yl)methyl acetate | IC50 | 179 nM | US-10278962: Tricyclic analogues, preparation method and uses thereof |
| [2-[(5aS,6S,8S,9aS,10R)-6-acetyloxy-10-hydroxy-5a-methyl-1-oxo-3-pyridin-3-yl-6,7,8,9,9a,10-hexahydropyrano[4,3-b]chromen-8-yl]-2-acetyloxypropyl] acetate | IC50 | 245 nM | US-10278962: Tricyclic analogues, preparation method and uses thereof |
| [(2R)-2-[(5aR,6R,8R,9aR,10S)-6-acetyloxy-10-hydroxy-5a-methyl-1-oxo-3-pyridin-3-yl-6,7,8,9,9a,10-hexahydropyrano[4,3-b]chromen-8-yl]-2-acetyloxypropyl] acetate | IC50 | 433 nM | US-10278962: Tricyclic analogues, preparation method and uses thereof |
| 2-[4-[2-(1H-benzimidazol-2-ylsulfanyl)ethyl]piperazin-1-yl]-N-[6-methyl-2,4-bis(methylsulfanyl)-3-pyridinyl]acetamide | IC50 | 450 nM | US-9149492: Method for selectively inhibiting ACAT1 in the treatment of alzheimer’s disease |
| (3R,6S,9S,13S)-9-benzyl-13-[(2S)-hexan-2-yl]-6-methyl-3-(2-methylpropyl)-1-oxa-4,7,10-triazacyclotridecane-2,5,8,11-tetrone | IC50 | 600 nM | US-9149492: Method for selectively inhibiting ACAT1 in the treatment of alzheimer’s disease |
| (3R,6S,9S,13S)-9-benzyl-3-[(2S)-butan-2-yl]-13-[(2S)-hexan-2-yl]-6-methyl-1-oxa-4,7,10-triazacyclotridecane-2,5,8,11-tetrone | IC50 | 900 nM | US-9149492: Method for selectively inhibiting ACAT1 in the treatment of alzheimer’s disease |
| [2-[(5aS,6S,8S,9aR)-6-(4-cyanobenzoyl)oxy-5a-methyl-1,10-dioxo-3-pyridin-3-yl-7,8,9,9a-tetrahydro-6H-pyrano[4,3-b]chromen-8-yl]-2-hydroxypropyl] 4-cyanobenzoate | IC50 | 17800 nM | US-10278962: Tricyclic analogues, preparation method and uses thereof |
| 1-[(1,3-diphenylpyrazol-5-yl)amino]decan-2-one | IC50 | 23000 nM | US-9149492: Method for selectively inhibiting ACAT1 in the treatment of alzheimer’s disease |
| 1-[(1,3-diphenylpyrazol-5-yl)amino]nonan-2-one | IC50 | 24000 nM | US-9149492: Method for selectively inhibiting ACAT1 in the treatment of alzheimer’s disease |
| N-decyl-1,3-diphenylpyrazol-5-amine | IC50 | 39000 nM | US-9149492: Method for selectively inhibiting ACAT1 in the treatment of alzheimer’s disease |
| [(2R)-2-[(5aR,6R,8R,9aR,10R)-6-acetyloxy-10-hydroxy-5a-methyl-1-oxo-3-pyridin-3-yl-6,7,8,9,9a,10-hexahydropyrano[4,3-b]chromen-8-yl]-2-acetyloxypropyl] acetate | IC50 | 56700 nM | US-10278962: Tricyclic analogues, preparation method and uses thereof |
| N-(2-phenylphenyl)octanamide | IC50 | 61000 nM | US-9149492: Method for selectively inhibiting ACAT1 in the treatment of alzheimer’s disease |
| [(5aS,6S,8S,9aS,10S)-10-acetyloxy-8-(1,2-diacetyloxypropan-2-yl)-5a-methyl-1-oxo-3-pyridin-3-yl-6,7,8,9,9a,10-hexahydropyrano[4,3-b]chromen-6-yl] 4-cyanobenzoate | IC50 | 64700 nM | US-10278962: Tricyclic analogues, preparation method and uses thereof |
| N-(2-phenylphenyl)nonanamide | IC50 | 65000 nM | US-9149492: Method for selectively inhibiting ACAT1 in the treatment of alzheimer’s disease |
| [(2R)-2-[(5aR,6R,8R,9aS,10S)-6-acetyloxy-10-hydroxy-5a-methyl-1-oxo-3-pyridin-3-yl-6,7,8,9,9a,10-hexahydropyrano[4,3-b]chromen-8-yl]-2-acetyloxypropyl] acetate | IC50 | 87400 nM | US-10278962: Tricyclic analogues, preparation method and uses thereof |
| [2-[(5aS,6S,8S,9aS,10S)-6-acetyloxy-10-hydroxy-5a-methyl-1-oxo-3-pyridin-3-yl-6,7,8,9,9a,10-hexahydropyrano[4,3-b]chromen-8-yl]-2-acetyloxypropyl] acetate | IC50 | 108000 nM | US-10278962: Tricyclic analogues, preparation method and uses thereof |
| [2-[(5aS,6S,8S,9aR)-6-hydroxy-5a-methyl-1,10-dioxo-3-pyridin-3-yl-7,8,9,9a-tetrahydro-6H-pyrano[4,3-b]chromen-8-yl]-2-hydroxypropyl] 4-cyanobenzoate | IC50 | 154000 nM | US-10278962: Tricyclic analogues, preparation method and uses thereof |
ChEMBL bioactivities
193 potent at pChembl≥5 of 227 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
PubChem BioAssay actives
151 with measured affinity, of 244 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.
| Compound | Assay | Type | Value | Unit |
|---|---|---|---|---|
| [(1S,2S,5S,6R,7R,9S,10S,18R)-5-acetyloxy-6-(acetyloxymethyl)-18-hydroxy-2,6,10-trimethyl-16-oxo-14-pyridin-3-yl-11,15-dioxatetracyclo[8.8.0.02,7.012,17]octadeca-12(17),13-dien-9-yl] 4-methoxybenzoate | 732688: Inhibition of ACAT2 (unknown origin) expressed in CHO cells | ic50 | 0.0008 | uM |
| [(1S,2S,5S,6R,7R,9S,10S,18R)-5-acetyloxy-6-(acetyloxymethyl)-18-hydroxy-2,6,10-trimethyl-16-oxo-14-pyridin-3-yl-11,15-dioxatetracyclo[8.8.0.02,7.012,17]octadeca-12(17),13-dien-9-yl] 4-methylbenzoate | 732688: Inhibition of ACAT2 (unknown origin) expressed in CHO cells | ic50 | 0.0009 | uM |
| [(1S,2S,5S,6R,7R,9S,10S,18R)-5-acetyloxy-6-(acetyloxymethyl)-18-hydroxy-2,6,10-trimethyl-16-oxo-14-pyridin-3-yl-11,15-dioxatetracyclo[8.8.0.02,7.012,17]octadeca-12(17),13-dien-9-yl] 4-cyanobenzoate | 1940249: Inhibition of SOAT2 (unknown origin) expressed in CHO cells using [14C]oleic acid incubated for 6 hrs | ic50 | 0.0009 | uM |
| [(1S,2S,5S,6R,7R,9S,10S,18R)-5-acetyloxy-6-(acetyloxymethyl)-18-hydroxy-2,6,10-trimethyl-16-oxo-14-pyridin-3-yl-11,15-dioxatetracyclo[8.8.0.02,7.012,17]octadeca-12(17),13-dien-9-yl] 3-fluorobenzoate | 732688: Inhibition of ACAT2 (unknown origin) expressed in CHO cells | ic50 | 0.0009 | uM |
| [(1S,2S,5S,6R,7R,9S,10S,18R)-5-acetyloxy-6-(acetyloxymethyl)-18-hydroxy-2,6,10-trimethyl-16-oxo-14-pyridin-3-yl-11,15-dioxatetracyclo[8.8.0.02,7.012,17]octadeca-12(17),13-dien-9-yl] 4-chlorobenzoate | 732688: Inhibition of ACAT2 (unknown origin) expressed in CHO cells | ic50 | 0.0010 | uM |
| [(1S,2S,5S,6R,7R,9S,10S,18R)-5-acetyloxy-6-(acetyloxymethyl)-18-hydroxy-2,6,10-trimethyl-16-oxo-14-pyridin-3-yl-11,15-dioxatetracyclo[8.8.0.02,7.012,17]octadeca-12(17),13-dien-9-yl] 4-ethylbenzoate | 732688: Inhibition of ACAT2 (unknown origin) expressed in CHO cells | ic50 | 0.0010 | uM |
| [(1S,2S,5S,6R,7R,9S,10S,18R)-5-acetyloxy-6-(acetyloxymethyl)-18-hydroxy-2,6,10-trimethyl-16-oxo-14-pyridin-3-yl-11,15-dioxatetracyclo[8.8.0.02,7.012,17]octadeca-12(17),13-dien-9-yl] 3-bromobenzoate | 732688: Inhibition of ACAT2 (unknown origin) expressed in CHO cells | ic50 | 0.0012 | uM |
| [(1S,2S,5S,6R,7R,9S,10S,18R)-5-acetyloxy-6-(acetyloxymethyl)-18-hydroxy-2,6,10-trimethyl-16-oxo-14-pyridin-3-yl-11,15-dioxatetracyclo[8.8.0.02,7.012,17]octadeca-12(17),13-dien-9-yl] 4-fluorobenzoate | 732688: Inhibition of ACAT2 (unknown origin) expressed in CHO cells | ic50 | 0.0017 | uM |
| [(1S,2S,5S,6R,7R,9S,10S,18R)-5-acetyloxy-6-(acetyloxymethyl)-18-hydroxy-2,6,10-trimethyl-16-oxo-14-pyridin-3-yl-11,15-dioxatetracyclo[8.8.0.02,7.012,17]octadeca-12(17),13-dien-9-yl] 4-bromobenzoate | 732688: Inhibition of ACAT2 (unknown origin) expressed in CHO cells | ic50 | 0.0020 | uM |
| [(1S,2S,5S,6R,7R,9S,10S,18R)-5-acetyloxy-6-(acetyloxymethyl)-18-hydroxy-2,6,10-trimethyl-16-oxo-14-pyridin-3-yl-11,15-dioxatetracyclo[8.8.0.02,7.012,17]octadeca-12(17),13-dien-9-yl] 4-methylsulfanylbenzoate | 732688: Inhibition of ACAT2 (unknown origin) expressed in CHO cells | ic50 | 0.0027 | uM |
| [(1S,2S,5S,6R,7R,9S,10S,18R)-5-acetyloxy-6-(acetyloxymethyl)-18-hydroxy-2,6,10-trimethyl-16-oxo-14-pyridin-3-yl-11,15-dioxatetracyclo[8.8.0.02,7.012,17]octadeca-12(17),13-dien-9-yl] 4-iodobenzoate | 732688: Inhibition of ACAT2 (unknown origin) expressed in CHO cells | ic50 | 0.0040 | uM |
| [(1S,2S,5S,6R,7R,9S,10S,18R)-5-acetyloxy-6-(acetyloxymethyl)-18-hydroxy-2,6,10-trimethyl-16-oxo-14-pyridin-3-yl-11,15-dioxatetracyclo[8.8.0.02,7.012,17]octadeca-12(17),13-dien-9-yl] 4-azidobenzoate | 732688: Inhibition of ACAT2 (unknown origin) expressed in CHO cells | ic50 | 0.0050 | uM |
| [(1S,2S,5S,6R,7R,9S,10S,18R)-5-acetyloxy-6-(acetyloxymethyl)-18-hydroxy-2,6,10-trimethyl-16-oxo-14-pyridin-3-yl-11,15-dioxatetracyclo[8.8.0.02,7.012,17]octadeca-12(17),13-dien-9-yl] 4-bromo-3-fluorobenzoate | 732688: Inhibition of ACAT2 (unknown origin) expressed in CHO cells | ic50 | 0.0050 | uM |
| [(1S,2S,5S,6R,7R,9S,10S,18R)-5-acetyloxy-6-(acetyloxymethyl)-18-hydroxy-2,6,10-trimethyl-16-oxo-14-pyridin-3-yl-11,15-dioxatetracyclo[8.8.0.02,7.012,17]octadeca-12(17),13-dien-9-yl] 4-nitrobenzoate | 1940249: Inhibition of SOAT2 (unknown origin) expressed in CHO cells using [14C]oleic acid incubated for 6 hrs | ic50 | 0.0050 | uM |
| [(1S,2S,5S,6R,7R,9S,10S,18R)-5-acetyloxy-6-(acetyloxymethyl)-18-hydroxy-2,6,10-trimethyl-16-oxo-14-pyridin-3-yl-11,15-dioxatetracyclo[8.8.0.02,7.012,17]octadeca-12(17),13-dien-9-yl] 4-ethenylbenzoate | 732688: Inhibition of ACAT2 (unknown origin) expressed in CHO cells | ic50 | 0.0050 | uM |
| [(1S,2S,5S,6R,7R,9S,10S,18R)-5-acetyloxy-6-(acetyloxymethyl)-18-hydroxy-2,6,10-trimethyl-16-oxo-14-pyridin-3-yl-11,15-dioxatetracyclo[8.8.0.02,7.012,17]octadeca-12(17),13-dien-9-yl] 3-methylbenzoate | 732688: Inhibition of ACAT2 (unknown origin) expressed in CHO cells | ic50 | 0.0050 | uM |
| [(1S,2S,5S,6R,7R,9S,10S,18R)-5-acetyloxy-6-(acetyloxymethyl)-18-hydroxy-2,6,10-trimethyl-16-oxo-14-pyridin-3-yl-11,15-dioxatetracyclo[8.8.0.02,7.012,17]octadeca-12(17),13-dien-9-yl] 3-iodobenzoate | 732688: Inhibition of ACAT2 (unknown origin) expressed in CHO cells | ic50 | 0.0050 | uM |
| [(1S,2S,5S,6R,7R,9S,10S,18R)-5-acetyloxy-6-(acetyloxymethyl)-18-hydroxy-2,6,10-trimethyl-16-oxo-14-pyridin-3-yl-11,15-dioxatetracyclo[8.8.0.02,7.012,17]octadeca-12(17),13-dien-9-yl] 2-iodobenzoate | 732688: Inhibition of ACAT2 (unknown origin) expressed in CHO cells | ic50 | 0.0050 | uM |
| [(1S,2S,5S,6R,7R,9S,10S,18R)-18-hydroxy-2,6,10-trimethyl-16-oxo-5-propanoyloxy-6-(propanoyloxymethyl)-14-pyridin-3-yl-11,15-dioxatetracyclo[8.8.0.02,7.012,17]octadeca-12(17),13-dien-9-yl] 4-cyanobenzoate | 744809: Inhibition of ACAT2 (unknown origin) | ic50 | 0.0056 | uM |
| [(1S,2S,5S,6R,7R,9S,10S,18R)-5-acetyloxy-6-(acetyloxymethyl)-18-hydroxy-2,6,10-trimethyl-16-oxo-14-pyridin-3-yl-11,15-dioxatetracyclo[8.8.0.02,7.012,17]octadeca-12(17),13-dien-9-yl] 3-fluoro-4-nitrobenzoate | 732688: Inhibition of ACAT2 (unknown origin) expressed in CHO cells | ic50 | 0.0060 | uM |
| [(1S,2S,3R,11S,12S,14R,15R,18R,20S)-3-hydroxy-1,11,15-trimethyl-5-oxo-18-phenyl-7-pyridin-3-yl-6,10,17,19-tetraoxapentacyclo[12.8.0.02,11.04,9.015,20]docosa-4(9),7-dien-12-yl] 4-cyanobenzoate | 755668: Inhibition of ACAT2 (unknown origin) | ic50 | 0.0060 | uM |
| [(1S,2S,5S,6R,7R,9S,10S,18R)-5-acetyloxy-6-(acetyloxymethyl)-18-hydroxy-2,6,10-trimethyl-16-oxo-14-pyridin-3-yl-11,15-dioxatetracyclo[8.8.0.02,7.012,17]octadeca-12(17),13-dien-9-yl] 3-fluoro-4-methoxybenzoate | 732688: Inhibition of ACAT2 (unknown origin) expressed in CHO cells | ic50 | 0.0061 | uM |
| [(1S,2S,5S,6R,7R,9S,10S,18R)-5-acetyloxy-6-(acetyloxymethyl)-18-hydroxy-2,6,10-trimethyl-16-oxo-14-pyridin-3-yl-11,15-dioxatetracyclo[8.8.0.02,7.012,17]octadeca-12(17),13-dien-9-yl] 3-fluoro-4-methylbenzoate | 732688: Inhibition of ACAT2 (unknown origin) expressed in CHO cells | ic50 | 0.0063 | uM |
| [(1S,2S,5S,6R,7R,9S,10S,18R)-18-hydroxy-2,6,10-trimethyl-5-(2-methylpropanoyloxy)-6-(2-methylpropanoyloxymethyl)-16-oxo-14-pyridin-3-yl-11,15-dioxatetracyclo[8.8.0.02,7.012,17]octadeca-12(17),13-dien-9-yl] 4-cyanobenzoate | 744809: Inhibition of ACAT2 (unknown origin) | ic50 | 0.0065 | uM |
| [(1S,2S,3R,11S,12S,14R,15R,18R,20S)-18-(2,4-dimethylphenyl)-3-hydroxy-1,11,15-trimethyl-5-oxo-7-pyridin-3-yl-6,10,17,19-tetraoxapentacyclo[12.8.0.02,11.04,9.015,20]docosa-4(9),7-dien-12-yl] 4-cyanobenzoate | 755668: Inhibition of ACAT2 (unknown origin) | ic50 | 0.0066 | uM |
| [(1S,2S,3R,11S,12S,14R,15R,18R,20S)-18-(2-fluorophenyl)-3-hydroxy-1,11,15-trimethyl-5-oxo-7-pyridin-3-yl-6,10,17,19-tetraoxapentacyclo[12.8.0.02,11.04,9.015,20]docosa-4(9),7-dien-12-yl] 4-cyanobenzoate | 755668: Inhibition of ACAT2 (unknown origin) | ic50 | 0.0068 | uM |
| [(1S,2S,5S,6R,7R,9S,10S,18R)-5-acetyloxy-6-(acetyloxymethyl)-18-hydroxy-2,6,10-trimethyl-16-oxo-14-pyridin-3-yl-11,15-dioxatetracyclo[8.8.0.02,7.012,17]octadeca-12(17),13-dien-9-yl] 4-bromo-2-fluorobenzoate | 732688: Inhibition of ACAT2 (unknown origin) expressed in CHO cells | ic50 | 0.0070 | uM |
| [(1S,2S,5S,6R,7R,9S,10S,18R)-5-acetyloxy-6-(acetyloxymethyl)-18-hydroxy-2,6,10-trimethyl-16-oxo-14-pyridin-3-yl-11,15-dioxatetracyclo[8.8.0.02,7.012,17]octadeca-12(17),13-dien-9-yl] 3-chlorobenzoate | 732688: Inhibition of ACAT2 (unknown origin) expressed in CHO cells | ic50 | 0.0070 | uM |
| [(1S,2S,3R,11S,12S,14R,15R,18R,20S)-3-hydroxy-1,11,15-trimethyl-5-oxo-18-phenyl-7-pyridin-3-yl-6,10,17,19-tetraoxapentacyclo[12.8.0.02,11.04,9.015,20]docosa-4(9),7-dien-12-yl] 4-fluorobenzoate | 755668: Inhibition of ACAT2 (unknown origin) | ic50 | 0.0070 | uM |
| [(1S,2S,3R,11S,12S,14R,15R,18R,20S)-18-(2,6-dimethylphenyl)-3-hydroxy-1,11,15-trimethyl-5-oxo-7-pyridin-3-yl-6,10,17,19-tetraoxapentacyclo[12.8.0.02,11.04,9.015,20]docosa-4(9),7-dien-12-yl] 4-cyanobenzoate | 1940249: Inhibition of SOAT2 (unknown origin) expressed in CHO cells using [14C]oleic acid incubated for 6 hrs | ic50 | 0.0072 | uM |
| [(1S,2S,5S,6R,7R,9S,10S,18R)-5-acetyloxy-6-(acetyloxymethyl)-18-hydroxy-2,6,10-trimethyl-16-oxo-14-pyridin-3-yl-11,15-dioxatetracyclo[8.8.0.02,7.012,17]octadeca-12(17),13-dien-9-yl] 4-cyano-3-fluorobenzoate | 732688: Inhibition of ACAT2 (unknown origin) expressed in CHO cells | ic50 | 0.0078 | uM |
| [(1S,2S,3R,11S,12S,14R,15R,18R,20S)-3-hydroxy-1,11,15-trimethyl-18-(3-methylphenyl)-5-oxo-7-pyridin-3-yl-6,10,17,19-tetraoxapentacyclo[12.8.0.02,11.04,9.015,20]docosa-4(9),7-dien-12-yl] 4-cyanobenzoate | 755668: Inhibition of ACAT2 (unknown origin) | ic50 | 0.0078 | uM |
| [(1S,2S,5S,6R,7R,9S,10S,18R)-5-acetyloxy-6-(acetyloxymethyl)-18-hydroxy-2,6,10-trimethyl-16-oxo-14-pyridin-3-yl-11,15-dioxatetracyclo[8.8.0.02,7.012,17]octadeca-12(17),13-dien-9-yl] 2,3,4-trifluorobenzoate | 732688: Inhibition of ACAT2 (unknown origin) expressed in CHO cells | ic50 | 0.0081 | uM |
| [(1S,2S,5S,6R,7R,9S,10S,18R)-5-acetyloxy-6-(acetyloxymethyl)-18-hydroxy-2,6,10-trimethyl-16-oxo-14-pyridin-3-yl-11,15-dioxatetracyclo[8.8.0.02,7.012,17]octadeca-12(17),13-dien-9-yl] 3-methylsulfanylbenzoate | 732688: Inhibition of ACAT2 (unknown origin) expressed in CHO cells | ic50 | 0.0090 | uM |
| [(1S,2S,3R,11S,12S,14R,15R,18R,20S)-3-hydroxy-1,11,15-trimethyl-5-oxo-18-phenyl-7-pyridin-3-yl-6,10,17,19-tetraoxapentacyclo[12.8.0.02,11.04,9.015,20]docosa-4(9),7-dien-12-yl] 4-chlorobenzoate | 755668: Inhibition of ACAT2 (unknown origin) | ic50 | 0.0090 | uM |
| [(1S,2S,5S,6R,7R,9S,10S,18R)-5-acetyloxy-6-(acetyloxymethyl)-18-hydroxy-2,6,10-trimethyl-16-oxo-14-pyridin-3-yl-11,15-dioxatetracyclo[8.8.0.02,7.012,17]octadeca-12(17),13-dien-9-yl] 4-phenylbenzoate | 732688: Inhibition of ACAT2 (unknown origin) expressed in CHO cells | ic50 | 0.0095 | uM |
| [(1S,2S,5S,6R,7R,9S,10S,18R)-6-(acetyloxymethyl)-5-benzoyloxy-18-hydroxy-2,6,10-trimethyl-16-oxo-14-pyridin-3-yl-11,15-dioxatetracyclo[8.8.0.02,7.012,17]octadeca-12(17),13-dien-9-yl] 4-cyanobenzoate | 744809: Inhibition of ACAT2 (unknown origin) | ic50 | 0.0096 | uM |
| [(1S,2S,3R,11S,12S,14R,15R,18R,20S)-3-hydroxy-1,11,15-trimethyl-18-(4-methylphenyl)-5-oxo-7-pyridin-3-yl-6,10,17,19-tetraoxapentacyclo[12.8.0.02,11.04,9.015,20]docosa-4(9),7-dien-12-yl] 4-cyanobenzoate | 755668: Inhibition of ACAT2 (unknown origin) | ic50 | 0.0097 | uM |
| [(1S,2S,5S,6R,7R,9S,10S,18R)-5-acetyloxy-6-(acetyloxymethyl)-18-hydroxy-2,6,10-trimethyl-16-oxo-14-pyridin-3-yl-11,15-dioxatetracyclo[8.8.0.02,7.012,17]octadeca-12(17),13-dien-9-yl] benzoate | 732688: Inhibition of ACAT2 (unknown origin) expressed in CHO cells | ic50 | 0.0100 | uM |
| [(1S,2S,3R,11S,12S,14R,15R,18R,20S)-3-hydroxy-1,11,15-trimethyl-18-(2-methylphenyl)-5-oxo-7-pyridin-3-yl-6,10,17,19-tetraoxapentacyclo[12.8.0.02,11.04,9.015,20]docosa-4(9),7-dien-12-yl] pentanoate | 1940249: Inhibition of SOAT2 (unknown origin) expressed in CHO cells using [14C]oleic acid incubated for 6 hrs | ic50 | 0.0100 | uM |
| [(1S,2S,5S,6R,7R,9S,10S,18R)-5-acetyloxy-6-(acetyloxymethyl)-18-hydroxy-2,6,10-trimethyl-16-oxo-14-pyridin-3-yl-11,15-dioxatetracyclo[8.8.0.02,7.012,17]octadeca-12(17),13-dien-9-yl] 3-cyanobenzoate | 732688: Inhibition of ACAT2 (unknown origin) expressed in CHO cells | ic50 | 0.0100 | uM |
| [(1S,2S,5S,6R,7R,9S,10S,18R)-5-acetyloxy-6-(acetyloxymethyl)-18-hydroxy-2,6,10-trimethyl-16-oxo-14-pyridin-3-yl-11,15-dioxatetracyclo[8.8.0.02,7.012,17]octadeca-12(17),13-dien-9-yl] 2-methylbenzoate | 732688: Inhibition of ACAT2 (unknown origin) expressed in CHO cells | ic50 | 0.0100 | uM |
| [(1S,2S,5S,6R,7R,9S,10S,18R)-6-(acetyloxymethyl)-18-hydroxy-2,6,10-trimethyl-16-oxo-5-propanoyloxy-14-pyridin-3-yl-11,15-dioxatetracyclo[8.8.0.02,7.012,17]octadeca-12(17),13-dien-9-yl] 4-cyanobenzoate | 744809: Inhibition of ACAT2 (unknown origin) | ic50 | 0.0100 | uM |
| [(1S,2S,3R,11S,12S,14R,15R,18R,20S)-3-hydroxy-1,11,15-trimethyl-5-oxo-18-phenyl-7-pyridin-3-yl-6,10,17,19-tetraoxapentacyclo[12.8.0.02,11.04,9.015,20]docosa-4(9),7-dien-12-yl] 4-bromobenzoate | 755668: Inhibition of ACAT2 (unknown origin) | ic50 | 0.0100 | uM |
| [(1S,2S,5S,6R,7R,9S,10S,18R)-5-acetyloxy-6-(acetyloxymethyl)-18-hydroxy-2,6,10-trimethyl-16-oxo-14-pyridin-3-yl-11,15-dioxatetracyclo[8.8.0.02,7.012,17]octadeca-12(17),13-dien-9-yl] 3-ethenylbenzoate | 732688: Inhibition of ACAT2 (unknown origin) expressed in CHO cells | ic50 | 0.0110 | uM |
| [(1S,2S,3R,11S,12S,14R,15R,18R,20S)-3-hydroxy-1,11,15-trimethyl-18-(2-methylphenyl)-5-oxo-7-pyridin-3-yl-6,10,17,19-tetraoxapentacyclo[12.8.0.02,11.04,9.015,20]docosa-4(9),7-dien-12-yl] 4-cyanobenzoate | 1940249: Inhibition of SOAT2 (unknown origin) expressed in CHO cells using [14C]oleic acid incubated for 6 hrs | ic50 | 0.0115 | uM |
| [(1S,2S,3R,11S,12S,14R,15R,18R,20S)-3-hydroxy-1,11,15-trimethyl-5-oxo-18-phenyl-7-pyridin-3-yl-6,10,17,19-tetraoxapentacyclo[12.8.0.02,11.04,9.015,20]docosa-4(9),7-dien-12-yl] 3-fluorobenzoate | 755668: Inhibition of ACAT2 (unknown origin) | ic50 | 0.0130 | uM |
| [(1S,2S,3R,11S,12S,14R,15R,18R,20S)-3-hydroxy-1,11,15-trimethyl-5-oxo-18-phenyl-7-pyridin-3-yl-6,10,17,19-tetraoxapentacyclo[12.8.0.02,11.04,9.015,20]docosa-4(9),7-dien-12-yl] 4-methoxybenzoate | 755668: Inhibition of ACAT2 (unknown origin) | ic50 | 0.0140 | uM |
| [(1S,2S,5S,6R,7R,9S,10S,18R)-5-acetyloxy-18-hydroxy-2,6,10-trimethyl-16-oxo-6-(propanoyloxymethyl)-14-pyridin-3-yl-11,15-dioxatetracyclo[8.8.0.02,7.012,17]octadeca-12(17),13-dien-9-yl] 4-cyanobenzoate | 744809: Inhibition of ACAT2 (unknown origin) | ic50 | 0.0144 | uM |
| [(1S,2S,5S,6R,7R,9S,10S,18R)-5-acetyloxy-6-(acetyloxymethyl)-18-hydroxy-2,6,10-trimethyl-16-oxo-14-pyridin-3-yl-11,15-dioxatetracyclo[8.8.0.02,7.012,17]octadeca-12(17),13-dien-9-yl] 3-methoxybenzoate | 732688: Inhibition of ACAT2 (unknown origin) expressed in CHO cells | ic50 | 0.0150 | uM |
CTD chemical–gene interactions
24 total (human), top 24 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| Benzo(a)pyrene | decreases expression, increases methylation | 3 |
| Tetrachlorodibenzodioxin | decreases expression | 2 |
| aristolochic acid I | increases expression | 1 |
| bisphenol A | affects expression | 1 |
| kojic acid | increases expression | 1 |
| beta-lapachone | decreases expression | 1 |
| 4-(N-methyl-N-nitrosamino)-1-(3-pyridyl)-1-butanone | decreases expression | 1 |
| mono-(2-ethylhexyl)phthalate | decreases expression | 1 |
| tris(1,3-dichloro-2-propyl)phosphate | decreases expression | 1 |
| butyraldehyde | increases expression | 1 |
| periodate-oxidized adenosine | affects expression | 1 |
| S-(1,2-dichlorovinyl)cysteine | affects response to substance, increases expression | 1 |
| CGP 52608 | affects binding, increases reaction | 1 |
| Dust | decreases expression | 1 |
| Hydrogen Peroxide | affects expression | 1 |
| Lipopolysaccharides | affects response to substance, increases expression | 1 |
| Quercetin | decreases expression | 1 |
| Silicon Dioxide | increases expression | 1 |
| Urethane | decreases expression | 1 |
| Valproic Acid | affects expression | 1 |
| Cyclosporine | decreases expression | 1 |
| Aflatoxin B1 | affects methylation | 1 |
| Copper Sulfate | decreases expression | 1 |
| Vitamin K 3 | affects expression | 1 |
ChEMBL screening assays
50 unique, capped per target: 50 binding
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL1272846 | Binding | Inhibition of human ACAT2 expressed in CHO cells assessed as inhibition of [3H]oleate-induced cholesterol ester accumulation | The tomato saponin, esculeoside A. — J Nat Prod |
Clinical trials (associated diseases)
0 trials via MONDO — disease-level, not drug-specific.
Related Atlas pages
No linked Atlas pages yet — the cross-entity mesh grows as the corpus expands.