DGAT1

Summary

DGAT1 (diacylglycerol O-acyltransferase 1, HGNC:2843) is a protein-coding gene on chromosome 8q24.3, encoding Diacylglycerol O-acyltransferase 1 (O75907). Catalyzes the terminal and only committed step in triacylglycerol synthesis by using diacylglycerol and fatty acyl CoA as substrates.

This gene encodes an multipass transmembrane protein that functions as a key metabolic enzyme. The encoded protein catalyzes the conversion of diacylglycerol and fatty acyl CoA to triacylglycerol. This enzyme can also transfer acyl CoA to retinol. Activity of this protein may be associated with obesity and other metabolic diseases.

Source: NCBI Gene 8694 — RefSeq curated summary.

At a glance

• Gene–disease (curated): congenital diarrhea 7 with exudative enteropathy (Strong, GenCC)
• GWAS associations: 1
• Clinical variants (ClinVar): 779 total — 36 pathogenic, 34 likely-pathogenic
• Phenotypes (HPO): 11
• Druggable target: yes — 3 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_012079

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:2843
Approved symbol	DGAT1
Name	diacylglycerol O-acyltransferase 1
Location	8q24.3
Locus type	gene with protein product
Status	Approved
Aliases	ARGP1
Ensembl gene	ENSG00000185000
Ensembl biotype	protein_coding
OMIM	604900
Entrez	8694

Gene structure

Transcript identifiers

Ensembl transcripts: 17 — 11 protein_coding, 4 retained_intron, 2 protein_coding_CDS_not_defined

ENST00000332324, ENST00000524844, ENST00000524965, ENST00000525371, ENST00000527885, ENST00000528718, ENST00000531896, ENST00000620428, ENST00000875293, ENST00000875294, ENST00000875295, ENST00000875296, ENST00000875297, ENST00000920392, ENST00000920393, ENST00000965791, ENST00000965792

RefSeq mRNA: 1 — MANE Select: NM_012079 NM_012079

CCDS: CCDS6420

Canonical transcript exons

ENST00000528718 — 17 exons

Exon	Start	End
ENSE00001611196	144317022	144317109
ENSE00001712961	144317187	144317252
ENSE00002169371	144317544	144317588
ENSE00003468719	144318261	144318362
ENSE00003478900	144317914	144318017
ENSE00003483517	144317784	144317822
ENSE00003513382	144318461	144318566
ENSE00003527511	144317671	144317712
ENSE00003564010	144318699	144318751
ENSE00003584553	144321321	144321408
ENSE00003614222	144318835	144318920
ENSE00003630363	144318095	144318169
ENSE00003665487	144317333	144317445
ENSE00003715860	144316853	144316915
ENSE00003750953	144319028	144319068
ENSE00003751745	144314584	144316709
ENSE00003848756	144326437	144326852

Expression profiles

Bgee: expression breadth ubiquitous, 134 present calls, max score 99.46.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 32.7482 / max 3728.7393, expressed in 1820 samples.

FANTOM5 promoters (13 alternative TSS)

Promoter ID	TPM avg	Samples expressed
95642	20.8423	1803
95639	4.1247	1603
95643	3.4973	1500
95644	1.6723	1010
95641	0.9241	574
95640	0.4095	202
95633	0.3925	200
95630	0.2040	82
95629	0.1933	82
95628	0.1531	63

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
duodenum	UBERON:0002114	99.46	gold quality
mucosa of transverse colon	UBERON:0004991	98.64	gold quality
right adrenal gland cortex	UBERON:0035827	98.43	gold quality
right adrenal gland	UBERON:0001233	98.35	gold quality
small intestine Peyer’s patch	UBERON:0003454	98.23	gold quality
left adrenal gland cortex	UBERON:0035825	98.21	gold quality
left adrenal gland	UBERON:0001234	98.07	gold quality
small intestine	UBERON:0002108	97.97	gold quality
transverse colon	UBERON:0001157	97.37	gold quality
adrenal gland	UBERON:0002369	97.25	gold quality
left testis	UBERON:0004533	97.25	gold quality
right testis	UBERON:0004534	97.16	gold quality
apex of heart	UBERON:0002098	96.74	gold quality
lower esophagus mucosa	UBERON:0035834	96.42	gold quality
right lobe of liver	UBERON:0001114	96.23	gold quality
subcutaneous adipose tissue	UBERON:0002190	96.18	gold quality
intestine	UBERON:0000160	96.16	gold quality
testis	UBERON:0000473	95.89	gold quality
adipose tissue	UBERON:0001013	95.83	gold quality
colon	UBERON:0001155	95.80	gold quality
blood	UBERON:0000178	95.71	gold quality
granulocyte	CL:0000094	95.63	gold quality
right hemisphere of cerebellum	UBERON:0014890	95.58	gold quality
omental fat pad	UBERON:0010414	95.41	gold quality
hindlimb stylopod muscle	UBERON:0004252	95.40	gold quality
rectum	UBERON:0001052	95.19	gold quality
heart left ventricle	UBERON:0002084	95.16	gold quality
cerebellar hemisphere	UBERON:0002245	94.98	gold quality
cerebellum	UBERON:0002037	94.94	gold quality
cerebellar cortex	UBERON:0002129	94.94	gold quality

Single-cell (SCXA)

Detected in 1 experiment(s), a significant marker in 1.

Experiment	Marker?	Max mean expression
E-ANND-3	yes	9.82

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): PPARG

miRNA regulators (miRDB)

64 targeting DGAT1, 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-8485	100.00	77.57	4731
HSA-MIR-1252-5P	100.00	69.80	2774
HSA-MIR-6748-5P	100.00	65.81	1057
HSA-MIR-34A-5P	99.99	71.21	1784
HSA-MIR-449A	99.99	71.05	1776
HSA-MIR-34C-5P	99.97	70.45	1577
HSA-MIR-449B-5P	99.97	70.26	1580
HSA-MIR-3941	99.86	70.54	2735
HSA-MIR-383-3P	99.85	65.84	1359
HSA-MIR-765	99.84	68.24	2442
HSA-MIR-4319	99.76	69.83	2586
HSA-MIR-6764-5P	99.75	67.89	2304
HSA-MIR-4756-3P	99.62	66.30	1319
HSA-MIR-6132	99.60	65.83	1554
HSA-MIR-6836-5P	99.60	65.62	1538
HSA-MIR-1290	99.59	69.90	2079
HSA-MIR-1915-3P	99.58	66.79	1988
HSA-MIR-5004-3P	99.54	68.27	1371
HSA-MIR-486-3P	99.51	66.82	1901
HSA-MIR-4672	99.50	71.58	2893
HSA-MIR-3128	99.50	67.85	1258
HSA-MIR-4688	99.48	64.68	828
HSA-MIR-6743-5P	99.48	63.60	721
HSA-MIR-3922-3P	99.25	64.96	1136
HSA-MIR-6837-5P	99.25	65.47	1632
HSA-MIR-4685-5P	99.25	65.99	1563
HSA-MIR-6744-3P	99.22	64.41	972
HSA-MIR-4291	99.20	68.88	2969
HSA-MIR-6852-5P	99.17	66.69	2073
HSA-MIR-4292	99.16	65.57	1767

Literature-anchored findings (GeneRIF, showing 40)

• Polymorphism associated with alterations in body mass index, high density lipoprotein levels and blood pressure in Turkish women. (PMID:12123490)
• DGAT1 overexpression in murine white adipose tissue provides a model in which obesity does not impair glucose disposal (PMID:12401709)
• DGAT participates in the regulation of membrane lipid synthesis and lipid signaling, thereby playing an important role in modulating cell growth properties (PMID:14557275)
• Niacin selectively inhibited DGAT2 but not DGAT1 activity, but had no effect on the expression of DGAT1 and DGAT2 mRNA (PMID:15258194)
• increasing DGAT1, ACAT1, or ACAT2 expression stimulates the assembly and secretion of VLDL from liver cells (PMID:15308631)
• adipose overexpression of Dgat1 gene in transgenic mice leads to diet-inducible insulin resistance. (PMID:16306352)
• thiazolidinediones upregulate the adipocyte lipid storage genes DGAT and FAS but have no significant effect on LPL (PMID:16894240)
• Review summarizes current knowledge of DGAT1 and DGAT2 enzymes, focusing on new advances since the cloning of their genes, including possible roles in human health and diseases. (PMID:18757836)
• the acylation of acylglycerols by DGAT1 is important for dietary fat absorption in the intestine (PMID:18768481)
• Report visceral and subcutaneous adipose tissue diacylglycerol acyltransferase activity in humans. (PMID:19197254)
• Identify DGAT1 as an important protein that participates in the effect of HNF4A on hepatic secretion of triglyceride-rich lipoproteins. (PMID:20167659)
• The triglyceride-synthesizing enzyme diacylglycerol acyltransferase-1 (DGAT1) is identified as a key host factor for hepatitis C virus infection. (PMID:20935628)
• human small intestinal DGAT, which is mainly encoded by DGAT1, utilizes 1,2-DAG as the substrate to form TAG (PMID:21369919)
• DGAT1 belongs to the family of oligomeric membrane proteins that adopt a dual membrane topology. (PMID:21846726)
• a comprehensive evaluation of a small molecule inhibitor for DGAT1 and suggests that pharmacological inhibition of DGAT1 holds promise in treating diverse metabolic disorders. (PMID:21990351)
• describe distinct but synergistic roles of the two DGATs in an integrated pathway of TAG synthesis and secretion, with DGAT2 acting upstream of DGAT1 (PMID:22748069)
• results identify DGAT1 loss-of-function mutations as a rare cause of congenital diarrheal disorders (PMID:23114594)
• The structure-activity relationship studies of a novel series of carboxylic acid derivatives of pyridine-carboxamides as DGAT-1 inhibitors is described. (PMID:23317570)
• Diacylglycerol acyltransferase-1 localizes hepatitis C virus NS5A protein to lipid droplets and enhances NS5A interaction with the viral capsid core (PMID:23420847)
• the apparent lack of therapeutic window owing to GI side effects of AZD7687, particularly diarrhoea, makes the utility of DGAT1 inhibition as a novel treatment for diabetes and obesity questionable. (PMID:24118885)
• MGAT2 functions as a dimeric or tetrameric protein and selectively heterodimerizes with DGAT1 in mammalian cells (PMID:24573674)
• Downregulation of CLDN1 was associated with altered fatty acid homeostasis in the absence of DGAT1. (PMID:24899196)
• Data indicate no clinically relevant pharmacokinetic interaction between DGAT-1 inhibitor pradigastat and rosuvastatin. (PMID:25740267)
• DGAT1 expression is down-regulated in viral hepatitis-related cirrhosis. (PMID:26493024)
• A novel homozygous missense variant was identified in a family with protein losing enteropathy. A splice site mutation in intron 8 was identified in a second family with PLE. These cases of DGAT1 deficiency extend the molecular and phenotypic spectrum of PLE. (PMID:26883093)
• DGAT1 mutations result in a spectrum of diseases (PMID:28373485)
• data reveal an important role for DGAT activity and TG synthesis generally in averting ER stress and lipotoxicity, with specifically DGAT1 performing this function during stimulated lipolysis in adipocytes. (PMID:28768178)
• our findings indicate that inhibition of both DGAT1 and ABHD5 using siRNA leads to reduction in prostate cancer cell growth. (PMID:28877685)
• Study identified a large cohort of patients with congenital diarrheal disorders with mutations in DGAT1 that reduced expression of its product; dermal fibroblasts and intestinal organoids derived from these patients had altered lipid metabolism and were susceptible to lipid-induced cell death. Expression of full-length wildtype DGAT1 or DGAT2 restored normal lipid metabolism in these cells. (PMID:29604290)
• DGAT1 loss causes global changes in enterocyte polarized trafficking that could account for deficits in absorption seen in the patient with neonatal diarrhea. (PMID:30095213)
• Decreased DGAT1 activity can reduce circulating TG and liver TG. (PMID:30790345)
• DGAT1 Inhibitor Suppresses Prostate Tumor Growth and Migration by Regulating Intracellular Lipids and Non-Centrosomal MTOC Protein GM130. (PMID:30816200)
• Identified 1 patient with compound heterozygous CCBE1 and 2 with novel DGAT1 mutations in cohort of 9 Chinese children. Two of the 3 patients with DGAT1 mutations died, suggesting that this genotype is associated with an especially severe phenotype. (PMID:30853196)
• Genetic variants in DGAT1 cause diverse clinical presentations of malnutrition through a specific molecular mechanism. (PMID:31778854)
• cryo-electron microscopy structure of human DGAT1 in complex with an oleoyl-CoA substrate (PMID:32433610)
• structure of dimeric human DGAT1, a member of the membrane-bound O-acyltransferase (MBOAT) family, by cryo-electron microscopy at approximately 3.0 A resolution (PMID:32433611)
• Targeting DGAT1 Ameliorates Glioblastoma by Increasing Fat Catabolism and Oxidative Stress. (PMID:32559414)
• Up-regulation of DGAT1 in cancer tissues and tumor-infiltrating macrophages influenced survival of patients with gastric cancer. (PMID:33750350)
• Loss of ephrin B2 receptor (EPHB2) sets lipid rheostat by regulating proteins DGAT1 and ATGL inducing lipid droplet storage in prostate cancer cells. (PMID:33824421)
• DGAT1 Expression Promotes Ovarian Cancer Progression and Is Associated with Poor Prognosis. (PMID:34095320)

Cross-species orthologs

5 orthologs

Organism	Symbol	Gene ID
danio_rerio	dgat1a	ENSDARG00000103503
mus_musculus	Dgat1	ENSMUSG00000022555
rattus_norvegicus	Dgat1	ENSRNOG00000028711
drosophila_melanogaster	mdy	FBGN0004797
caenorhabditis_elegans		WBGENE00010408

Paralogs (2): SOAT1 (ENSG00000057252), SOAT2 (ENSG00000167780)

Protein

Protein identifiers

Diacylglycerol O-acyltransferase 1 — O75907 (reviewed: O75907)

Alternative names: ACAT-related gene product 1, Acyl-CoA retinol O-fatty-acyltransferase, Diglyceride acyltransferase

All UniProt accessions (2): O75907, A0A0A0MR74

UniProt curated annotations — full annotation on UniProt →

Function. Catalyzes the terminal and only committed step in triacylglycerol synthesis by using diacylglycerol and fatty acyl CoA as substrates. Highly expressed in epithelial cells of the small intestine and its activity is essential for the absorption of dietary fats. In liver, plays a role in esterifying exogenous fatty acids to glycerol, and is required to synthesize fat for storage. Also present in female mammary glands, where it produces fat in the milk. May be involved in VLDL (very low density lipoprotein) assembly. In contrast to DGAT2 it is not essential for survival. Functions as the major acyl-CoA retinol acyltransferase (ARAT) in the skin, where it acts to maintain retinoid homeostasis and prevent retinoid toxicity leading to skin and hair disorders. Exhibits additional acyltransferase activities, includin acyl CoA:monoacylglycerol acyltransferase (MGAT), wax monoester and wax diester synthases. Also able to use 1-monoalkylglycerol (1-MAkG) as an acyl acceptor for the synthesis of monoalkyl-monoacylglycerol (MAMAG).

Subunit / interactions. Homodimer or homotetramer; both forms have similar enzymatic activities.

Subcellular location. Endoplasmic reticulum membrane.

Disease relevance. Diarrhea 7, protein-losing enteropathy type (DIAR7) [MIM:615863] A life-threatening disease characterized by severe, intractable, watery diarrhea. The disease is caused by variants affecting the gene represented in this entry.

Activity regulation. XP620 is a selective DGAT1 inhibitor.

Domain organisation. The disordered N-terminal region is required for the diacylglycerol O-acyltransferase activity and may regulate enzymatic function via its interaction with the MBOAT fold. The MBOAT fold forms a reaction chamber in the endoplasmic reticulum membrane that encloses the active sites. The reaction chamber has a tunnel to the cytosolic side and its entrance recognizes the hydrophilic CoA motif of an acyl-CoA molecule. The chamber has separate entrances for each of the two substrates, acyl-CoA and 1,2-diacyl-sn-glycerol.

Pathway. Lipid metabolism; glycerolipid metabolism.

Similarity. Belongs to the membrane-bound acyltransferase family. Sterol o-acyltransferase subfamily.

RefSeq proteins (1): NP_036211* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR004299	MBOAT_fam	Family
IPR014371	Oat_ACAT_DAG_ARE	Family
IPR027251	Diacylglycerol_acylTrfase1	Family

Pfam: PF03062

Enzyme classification (BRENDA):

• EC 2.3.1.20 — diacylglycerol O-acyltransferase (BRENDA: 78 organisms, 288 substrates, 261 inhibitors, 50 Km, 1 kcat entries)

Substrate kinetics (BRENDA)

12 substrates with measured Km, best-characterized 12. Km ranges are aggregated across organisms/conditions.

Substrate	Km (mM)	Measurements
OLEOYL-COA	0.0005–0.667	20
PALMITOYL-COA	0.0007–0.39	6
DIOLEIN	0.028–0.714	2
SN-1,2-DIOLEIN	0.006–0.113	2
1,2-DIOLEIN	0.014	1
1,2-DIOLEOYL-SN-GLYCEROL	0.5971	1
11-CIS-RETINOL	0.0085	1
13-CIS-RETINOL	0.0188	1
ALL-TRANS-RETINOL	0.0099	1
OCTODECYL-COA	0.0105	1
PALMITOLEOYL-COA	0.0062	1
STEAROYL-COA	0.0086	1

Catalyzed reactions (Rhea), 12 shown:

• an acyl-CoA + a 1,2-diacyl-sn-glycerol = a triacyl-sn-glycerol + CoA (RHEA:10868)
• all-trans-retinol + an acyl-CoA = an all-trans-retinyl ester + CoA (RHEA:11488)
• 2-(9Z-octadecenoyl)-glycerol + (9Z)-octadecenoyl-CoA = 1,2-di-(9Z-octadecenoyl)-sn-glycerol + CoA (RHEA:37911)
• 1-(9Z-octadecenoyl)-glycerol + (9Z)-octadecenoyl-CoA = 1,2-di-(9Z-octadecenoyl)-glycerol + CoA (RHEA:37915)
• 2-(9Z-octadecenoyl)-glycerol + hexadecanoyl-CoA = 1-hexadecanoyl-2-(9Z-octadecenoyl)-sn-glycerol + CoA (RHEA:38071)
• 1,2-di-(9Z-octadecenoyl)-sn-glycerol + hexadecanoyl-CoA = 1,2-di-(9Z)-octadecenoyl-3-hexadecanoyl-sn-glycerol + CoA (RHEA:38163)
• hexadecan-1-ol + hexadecanoyl-CoA = hexadecyl hexadecanoate + CoA (RHEA:38167)
• hexadecane-1,2-diol + hexadecanoyl-CoA = 2-hydroxyhexadecyl hexadecanoate + CoA (RHEA:38171)
• all-trans-retinol + hexadecanoyl-CoA = all-trans-retinyl hexadecanoate + CoA (RHEA:38175)
• hexadecane-1,2-diol + 2 hexadecanoyl-CoA = 1,2-O,O-dihexadecanoyl-1,2-hexadecanediol + 2 CoA (RHEA:38211)
• 1,2-di-(9Z-octadecenoyl)-sn-glycerol + (9Z)-octadecenoyl-CoA = 1,2,3-tri-(9Z-octadecenoyl)-glycerol + CoA (RHEA:38219)
• 1-octadecanoyl-2-(5Z,8Z,11Z,14Z-eicosatetraenoyl)-sn-glycerol + (9Z)-octadecenoyl-CoA = 1-octadecanoyl-2-(5Z,8Z,11Z,14Z)-eicosatetraenoyl-3-(9Z)-octadecenoyl-sn-glycerol + CoA (RHEA:38307)

UniProt features (91 total): mutagenesis site 24, helix 21, topological domain 10, transmembrane region 9, region of interest 7, binding site 4, turn 4, strand 3, modified residue 2, chain 1, short sequence motif 1, compositionally biased region 1, active site 1, site 1, sequence variant 1, sequence conflict 1

Structure

Experimental structures (PDB)

5 structures.

PDB	Method	Resolution (Å)
6VYI	ELECTRON MICROSCOPY	3
6VP0	ELECTRON MICROSCOPY	3.1
6VZ1	ELECTRON MICROSCOPY	3.2
8ESM	ELECTRON MICROSCOPY	3.2
8ETM	ELECTRON MICROSCOPY	3.2

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-O75907-F1	81.86	0.53

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 (2): 415; 416 (important for catalytic activity)

Ligand- & substrate-binding residues (4): 374–382; 390; 404; 477

Post-translational modifications (2): 17, 18

Mutagenesis-validated functional residues (24):

Position	Phenotype
346	strongly reduced diacylglycerol o-acyltransferase activity.
371	decreased diacylglycerol o-acyltransferase activity.
375	slightly decreased diacylglycerol o-acyltransferase activity.
377	abolished diacylglycerol o-acyltransferase activity.
378	abolished diacylglycerol o-acyltransferase activity.
381	does not affect diacylglycerol o-acyltransferase activity.
381	decreased diacylglycerol o-acyltransferase activity.
382	decreased diacylglycerol o-acyltransferase activity.
385	decreased diacylglycerol o-acyltransferase activity.
386	slightly decreased diacylglycerol o-acyltransferase activity.
390	decreased diacylglycerol o-acyltransferase activity.
391	slightly decreased diacylglycerol o-acyltransferase activity.
400	decreased diacylglycerol o-acyltransferase activity.
404	does not affect diacylglycerol o-acyltransferase activity.
404	decreased diacylglycerol o-acyltransferase activity.
407	decreased diacylglycerol o-acyltransferase activity.
411	abolished diacylglycerol o-acyltransferase activity.
411	decreased diacylglycerol o-acyltransferase activity.
415	abolished diacylglycerol o-acyltransferase activity.
416	abolished diacylglycerol o-acyltransferase activity.
434	reduced diacylglycerol o-acyltransferase activity.
437	reduced diacylglycerol o-acyltransferase activity.
465	reduced diacylglycerol o-acyltransferase activity.
469	slightly decreased diacylglycerol o-acyltransferase activity.

Function

Pathways and Gene Ontology

Reactome pathways

3 pathways

ID	Pathway
R-HSA-1482883	Acyl chain remodeling of DAG and TAG
R-HSA-6798695	Neutrophil degranulation
R-HSA-75109	Triglyceride biosynthesis

MSigDB gene sets: 277 (showing top): REACTOME_INNATE_IMMUNE_SYSTEM, GOCC_SECRETORY_GRANULE, ENK_UV_RESPONSE_KERATINOCYTE_UP, GRAESSMANN_APOPTOSIS_BY_DOXORUBICIN_UP, ACEVEDO_NORMAL_TISSUE_ADJACENT_TO_LIVER_TUMOR_DN, DACOSTA_UV_RESPONSE_VIA_ERCC3_UP, GOBP_REGULATION_OF_HORMONE_LEVELS, GOBP_ORGANOPHOSPHATE_METABOLIC_PROCESS, GOBP_RETINOL_METABOLIC_PROCESS, GOBP_PROTEIN_LIPID_COMPLEX_ASSEMBLY, GOBP_NUCLEOBASE_CONTAINING_SMALL_MOLECULE_METABOLIC_PROCESS, GOBP_LIPID_HOMEOSTASIS, GOBP_GLYCEROLIPID_METABOLIC_PROCESS, GOBP_FATTY_ACYL_COA_METABOLIC_PROCESS, GOBP_FATTY_ACID_HOMEOSTASIS

GO Biological Process (12): monoacylglycerol biosynthetic process (GO:0006640), triglyceride metabolic process (GO:0006641), triglyceride biosynthetic process (GO:0019432), lipid storage (GO:0019915), very-low-density lipoprotein particle assembly (GO:0034379), long-chain fatty-acyl-CoA metabolic process (GO:0035336), diacylglycerol metabolic process (GO:0046339), fatty acid homeostasis (GO:0055089), retinoid metabolic process (GO:0001523), lipid metabolic process (GO:0006629), retinol metabolic process (GO:0042572), glycerolipid metabolic process (GO:0046486)

GO Molecular Function (8): 2-acylglycerol O-acyltransferase activity (GO:0003846), diacylglycerol O-acyltransferase activity (GO:0004144), acyltransferase activity (GO:0016746), identical protein binding (GO:0042802), retinol O-fatty-acyltransferase activity (GO:0050252), protein binding (GO:0005515), obsolete O-acyltransferase activity (GO:0008374), transferase activity (GO:0016740)

GO Cellular Component (5): endoplasmic reticulum membrane (GO:0005789), plasma membrane (GO:0005886), membrane (GO:0016020), specific granule membrane (GO:0035579), endoplasmic reticulum (GO:0005783)

Reactome top-level categories

Rollup of top-3 pathways:

Category	Pathways
Glycerophospholipid biosynthesis	1
Innate Immune System	1
Triglyceride metabolism	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
acylglycerol biosynthetic process	2
acylglycerol metabolic process	2
acylglycerol O-acyltransferase activity	2
monoacylglycerol metabolic process	1
triglyceride metabolic process	1
nutrient storage	1
plasma lipoprotein particle assembly	1
fatty-acyl-CoA metabolic process	1
lipid homeostasis	1
diterpenoid metabolic process	1
primary metabolic process	1
retinoid metabolic process	1
primary alcohol metabolic process	1
hormone metabolic process	1
olefinic compound metabolic process	1
lipid metabolic process	1
transferase activity	1
protein binding	1
acyltransferase activity, transferring groups other than amino-acyl groups	1
retinol metabolic process	1
binding	1
catalytic activity	1
organelle membrane	1
nuclear outer membrane-endoplasmic reticulum membrane network	1
endoplasmic reticulum subcompartment	1
membrane	1
cell periphery	1
cellular anatomical structure	1
secretory granule membrane	1
specific granule	1
cytoplasm	1
endomembrane system	1
intracellular membrane-bounded organelle	1

Protein interactions and networks

STRING

2286 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
DGAT1	DGAT2	Q96PD7	989
DGAT1	MOGAT1	Q96PD6	954
DGAT1	MOGAT2	Q3SYC2	926
DGAT1	MOGAT3	Q86VF5	882
DGAT1	ACSL3	O95573	867
DGAT1	ACSL1	P33121	852
DGAT1	ACSL5	Q9ULC5	832
DGAT1	ACSL6	Q9UKU0	821
DGAT1	ACSL4	O60488	819
DGAT1	CD36	P16671	816
DGAT1	SCARB1	Q8WTV0	802
DGAT1	AGPAT1	Q99943	802
DGAT1	SCARB2	Q14108	799
DGAT1	PNPLA2	Q96AD5	793
DGAT1	SCD	O00767	792

IntAct

67 interactions, top by confidence:

A	B	Type	Score
TRDN	TMEM223	psi-mi:“MI:0914”(association)	0.640
DGAT1	DGAT1	psi-mi:“MI:0407”(direct interaction)	0.630
DGAT1	CCR9	psi-mi:“MI:0915”(physical association)	0.550
SLC7A1	TMEM223	psi-mi:“MI:0914”(association)	0.530
C3AR1	TMEM120B	psi-mi:“MI:0914”(association)	0.530
GPR21	TMEM120B	psi-mi:“MI:0914”(association)	0.530
POMK	TMEM120B	psi-mi:“MI:0914”(association)	0.530
CXCR4	TMEM120B	psi-mi:“MI:0914”(association)	0.530
TMEM184A	SLC33A1	psi-mi:“MI:0914”(association)	0.530
SLC30A2	ESYT2	psi-mi:“MI:0914”(association)	0.530
DGAT1		psi-mi:“MI:0915”(physical association)	0.400
	DGAT1	psi-mi:“MI:0915”(physical association)	0.400
CD1A	DGAT1	psi-mi:“MI:0915”(physical association)	0.370
DGAT1	GABRA4	psi-mi:“MI:0915”(physical association)	0.370
	ESYT2	psi-mi:“MI:0914”(association)	0.350
ESR1	ESYT2	psi-mi:“MI:0914”(association)	0.350
ATP2B2	GPR89A	psi-mi:“MI:0914”(association)	0.350
	NBAS	psi-mi:“MI:0914”(association)	0.350
ATP2B2	ESYT2	psi-mi:“MI:0914”(association)	0.350
TTYH1	TMEM223	psi-mi:“MI:0914”(association)	0.350
TSPAN15	TMEM223	psi-mi:“MI:0914”(association)	0.350

BioGRID (54): DGAT1 (Affinity Capture-MS), DGAT1 (Proximity Label-MS), DGAT1 (Affinity Capture-MS), DGAT1 (Affinity Capture-MS), DGAT1 (Affinity Capture-MS), DGAT1 (Affinity Capture-MS), DGAT1 (Affinity Capture-MS), DGAT1 (Affinity Capture-MS), DGAT1 (Affinity Capture-Western), DGAT1 (Reconstituted Complex), DGAT1 (Proximity Label-MS), DGAT1 (Proximity Label-MS), DGAT1 (Affinity Capture-MS), DGAT1 (Two-hybrid), DGAT1 (Affinity Capture-MS)

ESM2 similar proteins: A2VE61, A5PLL7, A6QLM0, B1AZA5, B8BIM2, D3ZXD8, E9PTA2, O35052, O75907, O94759, P48631, P52848, P98191, Q02353, Q05B45, Q0P5C0, Q0VCJ8, Q2QZ14, Q3UHN9, Q4R4U1, Q4R766, Q5EA70, Q5HZE2, Q5R5F8, Q5R7B1, Q61115, Q6DD32, Q6NYY9, Q6P360, Q6PHN7, Q84VT2, Q8BFQ2, Q8C1E7, Q8GZC3, Q8MK44, Q8NBD8, Q8NBT3, Q8VWZ8, Q90693, Q91YD4

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

1 interactions.

A	Effect	B	Mechanism
959122-11-3	down-regulates	DGAT1	“chemical inhibition”

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 73 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.

GO biological processes:

GO term	Partners	Fold	FDR
calcium-mediated signaling	5	13.9×	8e-03
positive regulation of cytosolic calcium ion concentration	7	12.4×	8e-04

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	36
Likely pathogenic	34
Uncertain significance	199
Likely benign	445
Benign	27

Top pathogenic / likely-pathogenic (30)

Variant ID	HGVS	Classification
1070479	NM_012079.6(DGAT1):c.1094G>A (p.Trp365Ter)	Pathogenic
1338779	NM_012079.6(DGAT1):c.805_*341del (p.Arg269fs)	Pathogenic
139512	NM_012079.6(DGAT1):c.751+2T>C	Pathogenic
1444253	NM_012079.6(DGAT1):c.530_531del (p.Cys177fs)	Pathogenic
1445272	NM_012079.6(DGAT1):c.868C>T (p.Gln290Ter)	Pathogenic
1685694	NM_012079.6(DGAT1):c.719_737dup (p.Leu247fs)	Pathogenic
1934297	NM_012079.6(DGAT1):c.445C>T (p.Gln149Ter)	Pathogenic
1973965	NM_012079.6(DGAT1):c.1020G>A (p.Trp340Ter)	Pathogenic
2000452	NM_012079.6(DGAT1):c.1148del (p.Lys383fs)	Pathogenic
2725251	NM_012079.6(DGAT1):c.356_376delinsTGGTGGACCCCATCCAGGTGGTTTCTGGGACCCCATCC (p.Gln119fs)	Pathogenic
2761446	NM_012079.6(DGAT1):c.921dup (p.Met308fs)	Pathogenic
2771570	NM_012079.6(DGAT1):c.778_788del (p.Thr260fs)	Pathogenic
2778046	NM_012079.6(DGAT1):c.428_429del (p.Phe143fs)	Pathogenic
2778430	NM_012079.6(DGAT1):c.801del (p.Arg269fs)	Pathogenic
2788681	NM_012079.6(DGAT1):c.69_82dup (p.Glu28fs)	Pathogenic
2814788	NM_012079.6(DGAT1):c.134del (p.Asp45fs)	Pathogenic
2826549	NM_012079.6(DGAT1):c.788dup (p.Tyr263Ter)	Pathogenic
2837131	NM_012079.6(DGAT1):c.751+2T>G	Pathogenic
2842666	NM_012079.6(DGAT1):c.1190del (p.Gly397fs)	Pathogenic
2842689	NM_012079.6(DGAT1):c.1075del (p.Glu359fs)	Pathogenic
2852216	NM_012079.6(DGAT1):c.739del (p.Asn246_Leu247insTer)	Pathogenic
2881168	NM_012079.6(DGAT1):c.70_122del (p.Pro24fs)	Pathogenic
2955867	NM_012079.6(DGAT1):c.69_82del (p.Pro24fs)	Pathogenic
3000461	NM_012079.6(DGAT1):c.1152G>A (p.Trp384Ter)	Pathogenic
3245577	NC_000008.10:g.(?145550080)(145550299_?)del	Pathogenic
3255347	NM_012079.6(DGAT1):c.1202G>A (p.Trp401Ter)	Pathogenic
3622637	NM_012079.6(DGAT1):c.133del (p.Asp45fs)	Pathogenic
3638464	NM_012079.6(DGAT1):c.1238del (p.Phe413fs)	Pathogenic
3655309	NM_012079.6(DGAT1):c.843del (p.Ile282fs)	Pathogenic
3677072	NM_012079.6(DGAT1):c.367_368del (p.Leu123fs)	Pathogenic

SpliceAI

2469 predictions. Top by Δscore:

Variant	Effect	Δscore
8:144316705:GGGAT:G	acceptor_gain	1.0000
8:144316710:C:CA	acceptor_loss	1.0000
8:144316710:C:CC	acceptor_gain	1.0000
8:144316848:CTCA:C	donor_loss	1.0000
8:144316849:TCA:T	donor_loss	1.0000
8:144316850:CAC:C	donor_loss	1.0000
8:144316851:A:T	donor_loss	1.0000
8:144316852:C:CT	donor_loss	1.0000
8:144316911:AGGTA:A	acceptor_gain	1.0000
8:144316912:GGTA:G	acceptor_gain	1.0000
8:144316913:GTA:G	acceptor_gain	1.0000
8:144316914:TA:T	acceptor_gain	1.0000
8:144316915:ACT:A	acceptor_loss	1.0000
8:144316916:C:CC	acceptor_gain	1.0000
8:144316916:CT:C	acceptor_loss	1.0000
8:144316921:A:AC	acceptor_gain	1.0000
8:144316921:A:C	acceptor_gain	1.0000
8:144317018:TGAC:T	donor_loss	1.0000
8:144317019:GAC:G	donor_loss	1.0000
8:144317020:A:AC	donor_gain	1.0000
8:144317021:C:CC	donor_gain	1.0000
8:144317021:CCT:C	donor_gain	1.0000
8:144317105:AGTGT:A	acceptor_gain	1.0000
8:144317106:GTGT:G	acceptor_gain	1.0000
8:144317107:TGT:T	acceptor_gain	1.0000
8:144317108:GT:G	acceptor_gain	1.0000
8:144317109:TC:T	acceptor_loss	1.0000
8:144317110:C:CC	acceptor_gain	1.0000
8:144317110:CTG:C	acceptor_loss	1.0000
8:144317111:T:C	acceptor_loss	1.0000

AlphaMissense

3182 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
8:144316649:A:G	W458R	1.000
8:144316649:A:T	W458R	1.000
8:144317334:A:G	W365R	1.000
8:144317334:A:T	W365R	1.000
8:144317213:G:C	N378K	0.999
8:144317213:G:T	N378K	0.999
8:144317218:A:G	W377R	0.999
8:144317218:A:T	W377R	0.999
8:144317227:A:G	W374R	0.999
8:144317227:A:T	W374R	0.999
8:144317249:G:C	N366K	0.999
8:144317249:G:T	N366K	0.999
8:144317252:C:A	W365C	0.999
8:144317252:C:G	W365C	0.999
8:144317337:A:G	W364R	0.999
8:144317337:A:T	W364R	0.999
8:144317347:G:C	F360L	0.999
8:144317347:G:T	F360L	0.999
8:144317349:A:G	F360L	0.999
8:144317354:C:G	R358P	0.999
8:144317362:A:C	F355L	0.999
8:144317362:A:T	F355L	0.999
8:144317364:A:G	F355L	0.999
8:144317712:A:G	W299R	0.999
8:144317712:A:T	W299R	0.999
8:144321322:A:G	L96P	0.999
8:144321338:A:G	W91R	0.999
8:144321338:A:T	W91R	0.999
8:144321350:C:G	G87R	0.999
8:144316659:G:C	N454K	0.998

dbSNP variants (sampled 300 via entrez): RS1000216326 (8:144326620 C>A,G,T), RS1000268837 (8:144326811 G>A,C), RS1000558471 (8:144316572 G>A,C,T), RS1000632176 (8:144316757 G>A), RS1001160251 (8:144321132 C>T), RS1001298660 (8:144318659 A>G), RS1001463604 (8:144324142 C>T), RS1001832677 (8:144323865 G>C), RS1001868541 (8:144327663 C>T), RS1002068617 (8:144314637 G>A,C), RS1002226053 (8:144317694 G>A), RS1002873711 (8:144322716 C>T), RS1002902160 (8:144319632 T>C), RS1003101317 (8:144324937 G>A,C), RS1003346515 (8:144315255 C>T)

Disease associations

OMIM: gene MIM:604900 | disease phenotypes: MIM:614707, MIM:615863, MIM:613217

GenCC curated gene-disease

Disease	Classification	Inheritance
congenital diarrhea 7 with exudative enteropathy	Strong	Autosomal recessive

Mondo (3): Brown-Vialetto-van Laere syndrome 2 (MONDO:0013867), congenital diarrhea 7 with exudative enteropathy (MONDO:0014375), congenital diarrhea 5 with tufting enteropathy (MONDO:0013184)

Orphanet (4): RFVT3-related riboflavin transporter deficiency (Orphanet:572550), Riboflavin transporter deficiency (Orphanet:97229), Congenital chronic diarrhea with protein-losing enteropathy (Orphanet:329242), Congenital tufting enteropathy (Orphanet:92050)

HPO phenotypes

11 total (11 of 11 shown, HPO-id order):

HPO	Term
HP:0000007	Autosomal recessive inheritance
HP:0001508	Failure to thrive
HP:0002013	Vomiting
HP:0002014	Diarrhea
HP:0002243	Protein-losing enteropathy
HP:0003073	Hypoalbuminemia
HP:0003077	Hyperlipidemia
HP:0003124	Hypercholesterolemia
HP:0003623	Neonatal onset
HP:0011473	Villous atrophy
HP:0011848	Abdominal colic

GWAS associations

1 associations (top):

Study	Trait	p-value
GCST004858_12	Dupuytren’s disease	5.000000e-14

EFO canonical traits (1, from GWAS)

EFO ID	Trait name
EFO:0004229	Dupuytren Contracture

MeSH disease descriptors (1)

Descriptor	Name	Tree numbers
C567703	Diarrhea 5, With Tufting Enteropathy, Congenital (supp.)

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL6009 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

3 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 539 (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
CHEMBL2364624	PRADIGASTAT	3	303
CHEMBL1835919	PF-04620110	1	37
CHEMBL4297354	AZD-7687	1	199

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

GtoPdb / IUPHAR curated pharmacology

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

Target class: enzyme — 2.3.1.- Acyltransferases

Most potent curated ligand interactions (5 total), top 5:

Ligand	Action	Affinity	Parameter
compound 5B [PMID: 25349648]	Inhibition	8.41	pIC50
T863	Inhibition	7.82	pIC50
PF-04620110	Inhibition	7.72	pIC50
compound 23n [PMID: 24900877]	Inhibition	7.19	pIC50
AZD7687	Inhibition	7.1	pIC50

Binding affinities (BindingDB)

495 measured of 592 human assays (592 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
(2S)-2-[[(1S)-1-carboxy-5-[4-[2-[2-[2-[2-(2,4-dinitroanilino)ethoxy]ethoxy]ethoxy]ethoxymethyl]triazol-1-yl]pentyl]carbamoylamino]pentanedioic acid	KI	0.02 nM	US-9296708: Chimeric small molecules for the recruitment of antibodies to cancer cells
(2S)-2-[[(1S)-1-carboxy-5-[4-[2-[2-(2,4-dinitroanilino)ethoxy]ethoxymethyl]triazol-1-yl]pentyl]carbamoylamino]pentanedioic acid	KI	0.024 nM	US-9296708: Chimeric small molecules for the recruitment of antibodies to cancer cells
(2S)-2-[[(1S)-1-carboxy-5-[4-[2-(2,4-dinitroanilino)ethoxymethyl]triazol-1-yl]pentyl]carbamoylamino]pentanedioic acid	KI	0.047 nM	US-9296708: Chimeric small molecules for the recruitment of antibodies to cancer cells
(2S)-2-[[(1S)-1-carboxy-5-[4-[2-[2-(4-nitroanilino)ethoxy]ethoxymethyl]triazol-1-yl]pentyl]carbamoylamino]pentanedioic acid	KI	0.06 nM	US-9296708: Chimeric small molecules for the recruitment of antibodies to cancer cells
(2S)-2-[[(1S)-1-carboxy-5-[4-[(2,4-dinitroanilino)methyl]triazol-1-yl]pentyl]carbamoylamino]pentanedioic acid	KI	0.078 nM	US-9296708: Chimeric small molecules for the recruitment of antibodies to cancer cells
(2S)-2-[[(1S)-1-carboxy-5-[4-[2-[2-(2-nitroanilino)ethoxy]ethoxymethyl]triazol-1-yl]pentyl]carbamoylamino]pentanedioic acid	KI	0.078 nM	US-9296708: Chimeric small molecules for the recruitment of antibodies to cancer cells
(2S)-2-[[(1S)-1-carboxy-5-[4-[2-[2-[2-[2-[2-[2-(2,4-dinitroanilino)ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxymethyl]triazol-1-yl]pentyl]carbamoylamino]pentanedioic acid	KI	0.101 nM	US-9296708: Chimeric small molecules for the recruitment of antibodies to cancer cells
(2S)-2-[[(1S)-1-carboxy-5-[4-[2-[2-[2-[2-[2-[2-[2-[2-(2,4-dinitroanilino)ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxymethyl]triazol-1-yl]pentyl]carbamoylamino]pentanedioic acid	KI	0.145 nM	US-9296708: Chimeric small molecules for the recruitment of antibodies to cancer cells
4-amino-6-[1-(2-cyclopentyloxyphenyl)indol-5-yl]-7,8-dihydropyrimido[5,4-f][1,4]oxazepin-5-one	IC50	0.3 nM	US-10174049: Compounds as diacylglycerol acyltransferase inhibitors
4-amino-6-[1-(2-methoxyphenyl)indol-5-yl]-7,8-dihydropyrimido[5,4-f][1,4]oxazepin-5-one	IC50	0.3 nM	US-10385066: Compounds as diacylglycerol acyltransferase inhibitors
4-amino-6-[1-(3-methoxyphenyl)indol-5-yl]-7,8-dihydropyrimido[5,4-f][1,4]oxazepin-5-one	IC50	0.5 nM	US-10174049: Compounds as diacylglycerol acyltransferase inhibitors
4-amino-6-[1-[3-(trifluoromethoxy)phenyl]pyrrolo[2,3-b]pyridin-5-yl]-7,8-dihydropyrimido[5,4-f][1,4]oxazepin-5-one	IC50	0.5 nM	US-9738658: Compounds as diacylglycerol acyltransferase inhibitors
4-Amino-6-(1-(3-(trifluoromethoxy)phenyl)-1H-indol-5-yl)-7,8-dihydropyrimido[5,4-f][1,4]oxazepin-5(6H)-one	IC50	0.5 nM	US-9796729: Compounds as diacylglycerol acyltransferase inhibitors
4-chloro-6-[1-[3-(trifluoromethoxy)phenyl]indol-5-yl]-7,8-dihydropyrimido[5,4-f][1,4]oxazepin-5-one	IC50	0.5 nM	US-10385066: Compounds as diacylglycerol acyltransferase inhibitors
2,2-dimethyl-3-[[4-methyl-5-[4-[5-[1-(trifluoromethyl)cyclopropyl]-1H-imidazol-2-yl]phenyl]-2-pyridinyl]oxy]propanoic acid	IC50	0.63 nM	US-9302996: Continuous arycyclic compound
2,2-dimethyl-3-[[4-methyl-5-[5-methyl-6-[5-(trifluoromethyl)-1H-imidazol-2-yl]-3-pyridinyl]-2-pyridinyl]oxy]propanoic acid	IC50	0.7 nM	US-9302996: Continuous arycyclic compound
(2S)-2-[[(1S)-5-[4-[2-(2-anilinoethoxy)ethoxymethyl]triazol-1-yl]-1-carboxypentyl]carbamoylamino]pentanedioic acid	KI	0.73 nM	US-9296708: Chimeric small molecules for the recruitment of antibodies to cancer cells
1-[[5-[3-fluoro-4-[5-(trifluoromethyl)-1H-imidazol-2-yl]phenyl]-4-methyl-2-pyridinyl]oxymethyl]cyclobutane-1-carboxylic acid	IC50	0.75 nM	US-9302996: Continuous arycyclic compound
2-ethyl-2-[[5-[6-[5-(trifluoromethyl)-1H-imidazol-2-yl]-3-pyridinyl]-2-pyridinyl]oxymethyl]butanoic acid	IC50	0.76 nM	US-9302996: Continuous arycyclic compound
2,2-dimethyl-3-[[4-methyl-5-[3-methyl-4-[5-(trifluoromethyl)-1H-imidazol-2-yl]phenyl]-2-pyridinyl]oxy]propanoic acid	IC50	0.78 nM	US-9302996: Continuous arycyclic compound
2-chloro-3-[[1-[5-[5-(trifluoromethyl)-1H-imidazol-2-yl]-2-pyridinyl]piperidin-4-yl]methoxy]benzoic acid	IC50	0.78 nM	US-10308636: Aromatic heterocyclic compound
1-[[5-[3-chloro-4-[5-(trifluoromethyl)-1H-imidazol-2-yl]phenyl]-4-methyl-2-pyridinyl]oxymethyl]cyclobutane-1-carboxylic acid	IC50	0.82 nM	US-9302996: Continuous arycyclic compound
3-[[3-fluoro-5-[4-[5-(trifluoromethyl)-1H-imidazol-2-yl]phenyl]-2-pyridinyl]oxy]-2,2-dimethylpropanoic acid	IC50	0.87 nM	US-9302996: Continuous arycyclic compound
2-ethyl-2-[[5-[6-(5-phenyl-1H-imidazol-2-yl)-3-pyridinyl]pyrazin-2-yl]oxymethyl]butanoic acid	IC50	0.94 nM	US-10308636: Aromatic heterocyclic compound
3-[[5-[3-fluoro-4-[5-(trifluoromethyl)-1H-imidazol-2-yl]phenyl]-4-methyl-2-pyridinyl]oxy]-2,2-dimethylpropanoic acid	IC50	0.96 nM	US-9302996: Continuous arycyclic compound
(2S)-2-[[(1S)-1-carboxy-5-[4-[2-[2-(4-methoxyanilino)ethoxy]ethoxymethyl]triazol-1-yl]pentyl]carbamoylamino]pentanedioic acid	KI	0.97 nM	US-9296708: Chimeric small molecules for the recruitment of antibodies to cancer cells
3-[[5-[5-chloro-6-[5-(1,1,2,2,2-pentafluoroethyl)-1H-imidazol-2-yl]-3-pyridinyl]-4-methyl-2-pyridinyl]oxy]-2,2-dimethylpropanoic acid	IC50	1 nM	US-9302996: Continuous arycyclic compound
methyl 3-[[5-[4-[3-(4-methoxyphenyl)-1H-1,2,4-triazol-5-yl]phenyl]-2-pyridinyl]oxy]-2,2-dimethylpropanoate	IC50	1.1 nM	US-10308636: Aromatic heterocyclic compound
methyl 3-[[5-[4-[5-(4-cyanophenoxy)-1-(2-trimethylsilylethoxymethyl)-1,2,4-triazol-3-yl]phenyl]-2-pyridinyl]oxy]-2,2-dimethylpropanoate	IC50	1.1 nM	US-10308636: Aromatic heterocyclic compound
methyl 2,2-dimethyl-3-[[5-[4-[5-(2,2,3,3,3-pentafluoropropoxy)-1-(2-trimethylsilylethoxymethyl)-1,2,4-triazol-3-yl]phenyl]-2-pyridinyl]oxy]propanoate	IC50	1.1 nM	US-10308636: Aromatic heterocyclic compound
3-[[5-[3-chloro-4-[5-(trifluoromethyl)-1H-imidazol-2-yl]phenyl]-4-methyl-2-pyridinyl]oxy]-2,2-dimethylpropanoic acid	IC50	1.2 nM	US-9302996: Continuous arycyclic compound
3-[[5-[4-[5-(cyclopropylmethyl)-1H-imidazol-2-yl]phenyl]-4-methyl-2-pyridinyl]oxy]-2,2-dimethylpropanoic acid	IC50	1.2 nM	US-9302996: Continuous arycyclic compound
2-[4-[(2-fluorophenoxy)methyl]cyclohexyl]-5-[5-(trifluoromethyl)-1H-imidazol-2-yl]pyridine	IC50	1.2 nM	US-10308636: Aromatic heterocyclic compound
3-[[5-[5-chloro-6-[5-(trifluoromethyl)-1H-imidazol-2-yl]-3-pyridinyl]-4-methyl-2-pyridinyl]oxy]-2,2-dimethylpropanoic acid	IC50	1.3 nM	US-9302996: Continuous arycyclic compound
(2S)-2-[[(1S)-1-carboxy-5-[4-[2-[2-[2-(2-methoxyethoxy)ethoxy]ethoxy]ethoxymethyl]triazol-1-yl]pentyl]carbamoylamino]pentanedioic acid	KI	1.34 nM	US-9296708: Chimeric small molecules for the recruitment of antibodies to cancer cells
(2S)-2-[[(1S)-1-carboxy-5-[4-(methoxymethyl)triazol-1-yl]pentyl]carbamoylamino]pentanedioic acid	KI	1.35 nM	US-9296708: Chimeric small molecules for the recruitment of antibodies to cancer cells
2,2-dimethyl-3-[4-[5-[5-(trifluoromethyl)-1H-imidazol-2-yl]-2-pyridinyl]phenoxy]propanoic acid	IC50	1.4 nM	US-9302996: Continuous arycyclic compound
3-[[5-[5-fluoro-6-[5-(trifluoromethyl)-1H-imidazol-2-yl]-3-pyridinyl]-4-methyl-2-pyridinyl]oxy]-2,2-dimethylpropanoic acid	IC50	1.4 nM	US-9302996: Continuous arycyclic compound
3-[[5-[3-fluoro-4-[5-[1-(trifluoromethyl)cyclopropyl]-1H-imidazol-2-yl]phenyl]-4-methyl-2-pyridinyl]oxy]-2,2-dimethylpropanoic acid	IC50	1.5 nM	US-9302996: Continuous arycyclic compound
3-[[5-[3-fluoro-4-[5-(trifluoromethyl)-1H-imidazol-2-yl]phenyl]-2-pyridinyl]oxy]-2,2-dimethylpropanoic acid	IC50	1.5 nM	US-9302996: Continuous arycyclic compound
2-ethyl-2-[[5-[3-fluoro-4-[5-(trifluoromethyl)-1H-imidazol-2-yl]phenyl]-4-methyl-2-pyridinyl]oxymethyl]butanoic acid	IC50	1.5 nM	US-9302996: Continuous arycyclic compound
ethyl 2-methyl-3-[[1-[4-[4-(trifluoromethyl)-1-(2-trimethylsilylethoxymethyl)imidazol-2-yl]phenyl]piperidin-4-yl]methoxy]benzoate	IC50	1.5 nM	US-10308636: Aromatic heterocyclic compound
1-[[5-[5-chloro-6-[5-(trifluoromethyl)-1H-imidazol-2-yl]-3-pyridinyl]-4-methyl-2-pyridinyl]oxymethyl]cyclobutane-1-carboxylic acid	IC50	1.6 nM	US-9302996: Continuous arycyclic compound
1-[[5-[3-fluoro-4-[5-(trifluoromethyl)-1H-imidazol-2-yl]phenyl]-4-methyl-2-pyridinyl]oxymethyl]cyclopropane-1-carboxylic acid	IC50	1.6 nM	US-9302996: Continuous arycyclic compound
(2S)-2-[[(1S)-1-carboxy-5-[4-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-(2,4-dinitroanilino)ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxymethyl]triazol-1-yl]pentyl]carbamoylamino]pentanedioic acid	KI	1.65 nM	US-9296708: Chimeric small molecules for the recruitment of antibodies to cancer cells
2,2-dimethyl-3-[[4-methyl-5-[5-[5-(trifluoromethyl)-1H-imidazol-2-yl]pyrazin-2-yl]-2-pyridinyl]oxy]propanoic acid	IC50	1.7 nM	US-9302996: Continuous arycyclic compound
2,2-dimethyl-3-[[4-methyl-5-[2-[5-(trifluoromethyl)-1H-imidazol-2-yl]pyrimidin-5-yl]-2-pyridinyl]oxy]propanoic acid	IC50	1.7 nM	US-9302996: Continuous arycyclic compound
2-ethyl-2-[[5-[5-fluoro-6-[5-(trifluoromethyl)-1H-imidazol-2-yl]-3-pyridinyl]-4-methyl-2-pyridinyl]oxymethyl]butanoic acid	IC50	1.7 nM	US-9302996: Continuous arycyclic compound
2,2-dimethyl-3-[[4-methyl-5-[5-[5-(1,1,2,2,2-pentafluoroethyl)-1H-imidazol-2-yl]pyrazin-2-yl]-2-pyridinyl]oxy]propanoic acid	IC50	1.7 nM	US-9302996: Continuous arycyclic compound
4-amino-6-[1-(3-chloro-2-methoxyphenyl)indol-5-yl]-7,8-dihydropyrimido[5,4-f][1,4]oxazepin-5-one	IC50	1.7 nM	US-10174049: Compounds as diacylglycerol acyltransferase inhibitors

ChEMBL bioactivities

1839 potent at pChembl≥5 of 1863 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
10.70	Ki	0.02	nM	CHEMBL3785201
10.62	Ki	0.024	nM	CHEMBL3896316
10.33	Ki	0.047	nM	CHEMBL3924320
10.22	Ki	0.06	nM	CHEMBL3921693
10.11	Ki	0.078	nM	CHEMBL3901785
10.11	Ki	0.078	nM	CHEMBL3959542
10.00	Ki	0.101	nM	CHEMBL3930993
9.84	Ki	0.145	nM	CHEMBL3786507
9.52	IC50	0.3	nM	CHEMBL5790611
9.52	IC50	0.3	nM	CHEMBL5825430
9.34	IC50	0.46	nM	CHEMBL3785201
9.30	IC50	0.5	nM	CHEMBL2036730
9.30	IC50	0.5	nM	CHEMBL5884647
9.30	IC50	0.5	nM	CHEMBL5993952
9.30	IC50	0.5	nM	CHEMBL6034495
9.30	IC50	0.5	nM	CHEMBL5744228
9.27	IC50	0.54	nM	CHEMBL3896316
9.22	IC50	0.6	nM	CHEMBL2036730
9.20	IC50	0.63	nM	CHEMBL3969207
9.15	IC50	0.7	nM	CHEMBL3963843
9.15	IC50	0.7	nM	CHEMBL4585408
9.14	Ki	0.73	nM	CHEMBL3897166
9.12	IC50	0.76	nM	CHEMBL3922835
9.12	IC50	0.75	nM	CHEMBL3913687
9.11	IC50	0.78	nM	CHEMBL3929252
9.11	IC50	0.78	nM	CHEMBL5979101
9.09	IC50	0.82	nM	CHEMBL3921484
9.06	IC50	0.87	nM	CHEMBL3914327
9.03	IC50	0.94	nM	CHEMBL5989278
9.02	IC50	0.96	nM	CHEMBL3907562
9.01	Ki	0.97	nM	CHEMBL3976145
9.00	IC50	1	nM	CHEMBL3898541
9.00	IC50	1	nM	CHEMBL4176968
8.98	IC50	1.05	nM	CHEMBL3924320
8.96	IC50	1.1	nM	CHEMBL3037924
8.96	IC50	1.1	nM	CHEMBL6034289
8.96	IC50	1.1	nM	CHEMBL5926150
8.96	IC50	1.1	nM	CHEMBL5850270
8.92	IC50	1.2	nM	CHEMBL3969728
8.92	IC50	1.2	nM	CHEMBL3966083
8.92	IC50	1.2	nM	CHEMBL5864682
8.89	IC50	1.3	nM	CHEMBL2408620
8.89	IC50	1.3	nM	CHEMBL3919047
8.89	IC50	1.3	nM	CHEMBL4467163
8.89	IC50	1.3	nM	CHEMBL4453443
8.87	Ki	1.35	nM	CHEMBL3904903
8.87	Ki	1.34	nM	CHEMBL1234976
8.87	IC50	1.36	nM	CHEMBL3921693
8.85	IC50	1.4	nM	CHEMBL2408472
8.85	IC50	1.4	nM	CHEMBL3929034

PubChem BioAssay actives

1027 with measured affinity, of 1369 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
2-[4-[4-[[5-(3,4-difluoroanilino)-1,3,4-oxadiazole-2-carbonyl]amino]phenyl]cyclohexyl]acetic acid	665880: Inhibition of DGAT1-mediated triacylglycerol synthesis in human HuTu80 cells	ic50	0.0005	uM
3-[[5-[5-(6-chloro-1H-benzimidazol-2-yl)-2-pyridinyl]-2-pyridinyl]oxy]-2,2-dimethylpropanoic acid	1593773: Inhibition of human DGAT1	ic50	0.0007	uM
2-[(2S)-2-ethyl-1-oxo-6-[4-[[3-(trifluoromethyl)phenyl]carbamoylamino]phenyl]-3,4-dihydronaphthalen-2-yl]acetic acid	1350286: Inhibition of recombinant human DGAT1 expressed in baculovirus infected Sf9 insect microsomal membranes using C10-DAG and [3H]-labelled decanoyl-CoA as substrates pretreated for 30 mins in presence of C10-DAG followed by [3H]-labelled decanoyl-CoA addition measured after 60 mins by microbeta counting method	ic50	0.0010	uM
2-[4-[4-[5-(6-chloro-1H-benzimidazol-2-yl)-2-pyridinyl]phenyl]cyclohexyl]acetic acid	760484: Inhibition of human DGAT1	ic50	0.0011	uM
4-[[5-[5-(6-chloro-1H-benzimidazol-2-yl)-2-pyridinyl]-2-pyridinyl]oxy]benzoic acid	1593773: Inhibition of human DGAT1	ic50	0.0013	uM
4-[[5-[5-(5,6-difluoro-1H-benzimidazol-2-yl)-2-pyridinyl]-2-pyridinyl]oxy]cyclohexane-1-carboxylic acid	760484: Inhibition of human DGAT1	ic50	0.0013	uM
2-[4-[[5-[5-(6-chloro-1H-benzimidazol-2-yl)-2-pyridinyl]-2-pyridinyl]oxy]cyclohexyl]acetic acid	1593773: Inhibition of human DGAT1	ic50	0.0013	uM
4-[[5-[5-(6-chloro-1H-benzimidazol-2-yl)-2-pyridinyl]-2-pyridinyl]oxy]cyclohexane-1-carboxylic acid	1593773: Inhibition of human DGAT1	ic50	0.0015	uM
2-[4-[[5-[5-[6-(trifluoromethyl)-1H-benzimidazol-2-yl]-2-pyridinyl]-2-pyridinyl]oxy]cyclohexyl]acetic acid	1593773: Inhibition of human DGAT1	ic50	0.0016	uM
1-[[5-[5-(6-chloro-1H-benzimidazol-2-yl)-2-pyridinyl]-2-pyridinyl]oxymethyl]cyclobutane-1-carboxylic acid	1593773: Inhibition of human DGAT1	ic50	0.0017	uM
2-[4-[4-[4-(6-chloro-1H-benzimidazol-2-yl)phenyl]phenyl]cyclohexyl]acetic acid	1593773: Inhibition of human DGAT1	ic50	0.0017	uM
4-[[5-[5-[6-(trifluoromethyl)-1H-benzimidazol-2-yl]-2-pyridinyl]-2-pyridinyl]oxy]cyclohexane-1-carboxylic acid	760484: Inhibition of human DGAT1	ic50	0.0017	uM
2-[4-[[5-[5-(5,6-difluoro-1H-benzimidazol-2-yl)-2-pyridinyl]-2-pyridinyl]oxy]cyclohexyl]acetic acid	1593773: Inhibition of human DGAT1	ic50	0.0017	uM
2-[(2S)-6-[4-[(4-chlorophenyl)carbamoylamino]phenyl]-2-ethyl-1-oxo-3,4-dihydronaphthalen-2-yl]acetic acid	1350283: Inhibition of recombinant human DGAT1 expressed in baculovirus infected Sf9 insect microsomal membranes using C10-DAG and C10-CoA as substrate pretreated for 15 mins followed by substrate addition measured after 60 mins by CPM dye based fluorescence assay	ic50	0.0020	uM
2-[6-[4-[(4-chlorophenyl)carbamoylamino]phenyl]-2-ethyl-1-oxo-3,4-dihydronaphthalen-2-yl]acetic acid	1350283: Inhibition of recombinant human DGAT1 expressed in baculovirus infected Sf9 insect microsomal membranes using C10-DAG and C10-CoA as substrate pretreated for 15 mins followed by substrate addition measured after 60 mins by CPM dye based fluorescence assay	ic50	0.0020	uM
2-[4-[1-[5-[6-(trifluoromethyl)-1H-benzimidazol-2-yl]-2-pyridinyl]piperidin-4-yl]oxycyclohexyl]acetic acid	1593773: Inhibition of human DGAT1	ic50	0.0020	uM
(1R,5S)-3-[1-[5-[6-(trifluoromethyl)-1H-benzimidazol-2-yl]-2-pyridinyl]piperidin-4-yl]oxybicyclo[3.1.0]hexane-6-carboxylic acid	1524971: Inhibition of human DGAT1	ic50	0.0020	uM
4-[[5-[5-(6-fluoro-1H-benzimidazol-2-yl)-2-pyridinyl]-2-pyridinyl]oxy]cyclohexane-1-carboxylic acid	760484: Inhibition of human DGAT1	ic50	0.0020	uM
2-[4-[[5-[5-(4,6-difluoro-1H-benzimidazol-2-yl)-2-pyridinyl]-2-pyridinyl]oxy]cyclohexyl]acetic acid	1593773: Inhibition of human DGAT1	ic50	0.0021	uM
4-[1-[5-(6-chloro-1H-benzimidazol-2-yl)-2-pyridinyl]piperidin-4-yl]oxycyclohexane-1-carboxylic acid	1169964: Inhibition of human DGAT1	ic50	0.0022	uM
2-[4-[4-[4-[6-(trifluoromethyl)-1H-benzimidazol-2-yl]phenyl]phenyl]cyclohexyl]acetic acid	1593773: Inhibition of human DGAT1	ic50	0.0023	uM
2-[4-[[5-[5-(6-fluoro-1H-benzimidazol-2-yl)-2-pyridinyl]-2-pyridinyl]oxy]cyclohexyl]acetic acid	1593773: Inhibition of human DGAT1	ic50	0.0024	uM
1-[5-[5-(6-chloro-1H-benzimidazol-2-yl)-2-pyridinyl]-2-pyridinyl]-4-methylpiperidine-4-carboxylic acid	1593773: Inhibition of human DGAT1	ic50	0.0025	uM
4-[1-[5-[6-(trifluoromethyl)-1H-benzimidazol-2-yl]-2-pyridinyl]piperidin-4-yl]oxycyclohexane-1-carboxylic acid	1169964: Inhibition of human DGAT1	ic50	0.0025	uM
1-[[[5-[5-(6-chloro-1H-benzimidazol-2-yl)-2-pyridinyl]-2-pyridinyl]amino]methyl]cyclopropane-1-carboxylic acid	1593773: Inhibition of human DGAT1	ic50	0.0029	uM
2-[6-[4-amino-7,7-dimethyl-2-(trifluoromethyl)pyrimido[4,5-b][1,4]oxazin-6-yl]spiro[1,2-dihydroindene-3,4’-cyclohexane]-1’-yl]acetic acid	1126039: Inhibition of DGAT1 (unknown origin) by cell-based assay	ic50	0.0030	uM
4-[4-[(5-anilino-1,3,4-thiadiazol-2-yl)carbamoyl]phenoxy]cyclohexane-1-carboxylic acid	1266130: Inhibition of DGAT-1 in human Chang cells assessed as lipid level after 6 hrs in presence of substrate [14C]glycerol by HPLC analysis	ic50	0.0030	uM
2-[(2S)-6-[5-[(3,4-difluorophenyl)carbamoylamino]pyrazin-2-yl]-1-oxo-2-(2,2,2-trifluoroethyl)-3,4-dihydronaphthalen-2-yl]acetic acid	1350286: Inhibition of recombinant human DGAT1 expressed in baculovirus infected Sf9 insect microsomal membranes using C10-DAG and [3H]-labelled decanoyl-CoA as substrates pretreated for 30 mins in presence of C10-DAG followed by [3H]-labelled decanoyl-CoA addition measured after 60 mins by microbeta counting method	ic50	0.0030	uM
2-[(2S)-1-oxo-2-(2,2,2-trifluoroethyl)-6-[5-[[3-(trifluoromethyl)phenyl]carbamoylamino]pyrazin-2-yl]-3,4-dihydronaphthalen-2-yl]acetic acid	1350286: Inhibition of recombinant human DGAT1 expressed in baculovirus infected Sf9 insect microsomal membranes using C10-DAG and [3H]-labelled decanoyl-CoA as substrates pretreated for 30 mins in presence of C10-DAG followed by [3H]-labelled decanoyl-CoA addition measured after 60 mins by microbeta counting method	ic50	0.0030	uM
3-oxo-1’-[5-[6-(trifluoromethyl)-1H-benzimidazol-2-yl]-2-pyridinyl]spiro[2-benzofuran-1,4’-piperidine]-5-carboxylic acid	1481041: Inhibition of human DGAT1 expressed in yeast membrane fraction assessed as inhibition of triglyceride formation using diolein/oleoyl-CoA as substrate measured after 1 hr by 7-diethylamino-3-(4’-maleimidylphenyl)-4-methylcoumarin based fluorescence analysis	ic50	0.0030	uM
2-[1-oxo-6-[4-(phenylcarbamoylamino)phenyl]-2-(2,2,2-trifluoroethyl)-3,4-dihydronaphthalen-2-yl]acetic acid	1350283: Inhibition of recombinant human DGAT1 expressed in baculovirus infected Sf9 insect microsomal membranes using C10-DAG and C10-CoA as substrate pretreated for 15 mins followed by substrate addition measured after 60 mins by CPM dye based fluorescence assay	ic50	0.0030	uM
2-[2-ethyl-1-oxo-6-[4-[[3-(trifluoromethyl)phenyl]carbamoylamino]phenyl]-3,4-dihydronaphthalen-2-yl]acetic acid	1350283: Inhibition of recombinant human DGAT1 expressed in baculovirus infected Sf9 insect microsomal membranes using C10-DAG and C10-CoA as substrate pretreated for 15 mins followed by substrate addition measured after 60 mins by CPM dye based fluorescence assay	ic50	0.0030	uM
1-[[5-[5-(6-chloro-1H-benzimidazol-2-yl)-2-pyridinyl]-2-pyridinyl]oxymethyl]cyclopropane-1-carboxylic acid	1593773: Inhibition of human DGAT1	ic50	0.0031	uM
2-[4-[1-[5-(6-chloro-1H-benzimidazol-2-yl)-2-pyridinyl]piperidin-4-yl]oxycyclohexyl]acetic acid	1593773: Inhibition of human DGAT1	ic50	0.0031	uM
2-[4-[[5-[5-(6-chloro-1H-imidazo[4,5-b]pyridin-2-yl)-2-pyridinyl]-2-pyridinyl]oxy]cyclohexyl]acetic acid	1593773: Inhibition of human DGAT1	ic50	0.0032	uM
4-[[5-[5-(6-cyano-1H-benzimidazol-2-yl)-2-pyridinyl]-2-pyridinyl]oxy]cyclohexane-1-carboxylic acid	760484: Inhibition of human DGAT1	ic50	0.0032	uM
3-[[5-[5-(6-chloro-1H-benzimidazol-2-yl)-2-pyridinyl]-2-pyridinyl]oxy]cyclobutane-1-carboxylic acid	1593773: Inhibition of human DGAT1	ic50	0.0035	uM
2-[4-[4-[5-[6-(trifluoromethyl)-1H-benzimidazol-2-yl]-2-pyridinyl]phenyl]cyclohexyl]acetic acid	760484: Inhibition of human DGAT1	ic50	0.0035	uM
(2S)-1-[5-[4-[[3-(trifluoromethyl)phenyl]carbamoylamino]phenyl]pyridine-2-carbonyl]pyrrolidine-2-carboxylic acid	1461832: Inhibition of recombinant full length human DGAT1 expressed in Sf9 insect cells using 1,2-didecanoyl-sn-glycerol as substrate after 60 mins in presence of palmitoyl-1-14C coenzyme A by scintillation counting	ic50	0.0035	uM
2-[[5-[5-(6-chloro-1H-benzimidazol-2-yl)-2-pyridinyl]-2-pyridinyl]oxymethyl]cyclopropane-1-carboxylic acid	1593773: Inhibition of human DGAT1	ic50	0.0036	uM
2-[4-[[5-[5-(6-cyano-1H-benzimidazol-2-yl)-2-pyridinyl]-2-pyridinyl]oxy]cyclohexyl]acetic acid	1593773: Inhibition of human DGAT1	ic50	0.0036	uM
(2S)-1-[5-[4-[(3-chlorophenyl)carbamoylamino]phenyl]pyridine-2-carbonyl]pyrrolidine-2-carboxylic acid	1461832: Inhibition of recombinant full length human DGAT1 expressed in Sf9 insect cells using 1,2-didecanoyl-sn-glycerol as substrate after 60 mins in presence of palmitoyl-1-14C coenzyme A by scintillation counting	ic50	0.0037	uM
4-[[5-[5-[6-(trifluoromethoxy)-1H-benzimidazol-2-yl]-2-pyridinyl]-2-pyridinyl]oxy]cyclohexane-1-carboxylic acid	760484: Inhibition of human DGAT1	ic50	0.0039	uM
2,2-dimethyl-3-[[4-methyl-5-[4-(naphthalene-2-carbonylamino)phenyl]-1,2,4-triazol-3-yl]oxy]propanoic acid	639984: Inhibition of human recombinant N-terminus FLAG-tagged DGAT1 expressed in baculovirus infected insect Sf9 cells assessed as triglyceride synthesis	ic50	0.0040	uM
4-[[5-[5-(1H-benzimidazol-2-yl)-2-pyridinyl]-2-pyridinyl]oxy]cyclohexane-1-carboxylic acid	760484: Inhibition of human DGAT1	ic50	0.0040	uM
2-[4-[4-(4-amino-7,7-dimethylpyrimido[4,5-b][1,4]oxazin-6-yl)phenyl]cyclohexyl]acetic acid	1126039: Inhibition of DGAT1 (unknown origin) by cell-based assay	ic50	0.0040	uM
2-[4-[1-[5-(4,6-difluoro-1H-benzimidazol-2-yl)-2-pyridinyl]piperidin-4-yl]oxycyclohexyl]acetic acid	1593773: Inhibition of human DGAT1	ic50	0.0041	uM
2-[[5-[5-(6-chloro-1H-benzimidazol-2-yl)-2-pyridinyl]-2-pyridinyl]amino]cyclohexane-1-carboxylic acid	1593773: Inhibition of human DGAT1	ic50	0.0042	uM
2-[4-[4-[[5-(2-fluoroanilino)-1,3,4-oxadiazole-2-carbonyl]amino]phenyl]cyclohexyl]acetic acid	665873: Inhibition of human recombinant DGAT1 expressed in baculovirus infected insect sf9 cells using [14C] oleoyl coenzyme A after 30 mins by scintillation counting	ic50	0.0044	uM
1-[5-[5-(6-chloro-1H-benzimidazol-2-yl)-2-pyridinyl]-2-pyridinyl]-3-methylpiperidine-3-carboxylic acid	1593773: Inhibition of human DGAT1	ic50	0.0045	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
Benzo(a)pyrene	affects methylation, affects cotreatment, decreases expression	4
Cyclosporine	decreases expression, decreases methylation	4
bisphenol A	decreases reaction, increases expression, affects expression	3
Valproic Acid	affects expression, increases expression, increases methylation	3
Oleic Acid	affects cotreatment, decreases expression, decreases reaction, increases expression	3
Palmitic Acid	decreases reaction, increases expression, affects cotreatment, decreases expression	3
tris(1,3-dichloro-2-propyl)phosphate	increases expression, decreases expression	2
sodium arsenite	decreases expression	2
Cadmium	increases abundance, increases expression	2
Dichlorodiphenyl Dichloroethylene	decreases expression, increases expression	2
Aflatoxin B1	decreases expression, affects expression	2
aristolochic acid I	decreases expression	1
cinnabarinic acid	decreases reaction, increases expression	1
FR900359	increases phosphorylation	1
dicrotophos	decreases expression	1
methyleugenol	decreases expression	1
triphenyl phosphate	affects expression	1
beta-thujone	increases expression, affects cotreatment	1
benzo(b)fluoranthene	affects cotreatment, decreases expression	1
glycidyl methacrylate	decreases expression	1
tributyltin	affects cotreatment, increases expression	1
spathulenol	increases expression, affects cotreatment	1
sulforaphane	decreases reaction, increases expression	1
linalool	affects cotreatment, increases expression	1
perfluorooctanoic acid	increases expression	1
caryophyllene	affects cotreatment, increases expression	1
aflatoxin B2	increases methylation	1
benz(a)anthracene	affects cotreatment, decreases expression	1
chrysene	affects cotreatment, decreases expression	1
2-chloroethyl ethyl sulfide	increases expression	1

ChEMBL screening assays

130 unique, capped per target: 130 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1022199	Binding	Inhibition of human recombinant DGAT1 expressed in Sf9 cells by liquid scintillography	Discovery of a potent, selective, and orally efficacious pyrimidinooxazinyl bicyclooctaneacetic acid diacylglycerol acyltransferase-1 inhibitor. — J Med Chem

Cellosaurus cell lines

5 cell lines: 5 cancer cell line

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

Cellosaurus	Name	Category	Sex
CVCL_D1M8	Abcam K-562 DGAT1 KO	Cancer cell line	Female
CVCL_D2IT	Abcam Raji DGAT1 KO	Cancer cell line	Male
CVCL_E1VK	HAP1 DGAT1 (-) 1	Cancer cell line	Male
CVCL_E1VL	HAP1 DGAT1 (-) 2	Cancer cell line	Male
CVCL_UQ40	Abcam Jurkat DGAT1 KO	Cancer cell line	Male

Clinical trials (associated diseases)

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

Trial	Phase	Status	Title
NCT01114035	Not specified	COMPLETED	Characterization Phenotypic and Genetic Study of the Intestinal Epithelial Dysplasia or Tufting Enteropathy (TE)