LIPG

Summary

LIPG (lipase G, endothelial type, HGNC:6623) is a protein-coding gene on chromosome 18q21.1, encoding Endothelial lipase (Q9Y5X9). Exerts both phospholipase and triglyceride lipase activities.

The protein encoded by this gene has substantial phospholipase activity and may be involved in lipoprotein metabolism and vascular biology. This protein is designated a member of the TG lipase family by its sequence and characteristic lid region which provides substrate specificity for enzymes of the TG lipase family.

Source: NCBI Gene 9388 — RefSeq curated summary.

At a glance

• GWAS associations: 116 (top 1% of genes corpus-wide)
• Clinical variants (ClinVar): 244 total
• GTEx eGene: eQTL in 23 tissues, sQTL in 1 (q < 0.05)
• ChEMBL bioactivity: 1 clinical-phase molecule tested; no curated mechanism-of-action drug
• Constraint (gnomAD): pLI 0.00 (LoF-tolerant), LOEUF 0.88 (unconstrained)
• MANE Select transcript: NM_006033
• Notable: 244 clinical variants but no curated precision-oncology (CIViC) evidence yet

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:6623
Approved symbol	LIPG
Name	lipase G, endothelial type
Location	18q21.1
Locus type	gene with protein product
Status	Approved
Aliases	EDL
Ensembl gene	ENSG00000101670
Ensembl biotype	protein_coding
OMIM	603684
Entrez	9388

Gene structure

Transcript identifiers

Ensembl transcripts: 13 — 10 protein_coding, 1 non_stop_decay, 1 TEC, 1 nonsense_mediated_decay

MANE Select: ENST00000261292

Transcript support level (Ensembl TSL; 1 = fully mRNA-supported): TSL 1: 2, TSL 2: 3, TSL 3: 1

ENST00000261292, ENST00000427224, ENST00000577628, ENST00000579750, ENST00000580036, ENST00000583083, ENST00000623277, ENST00000931130, ENST00000959465, ENST00000984843, ENST00001082664, ENST00001082665, ENST00001124792

RefSeq mRNA: 2 — MANE Select: NM_006033 NM_001308006, NM_006033

CCDS: CCDS11938, CCDS77187

Canonical transcript exons

ENST00000261292 — 10 exons

Exon	Start	End
ENSE00001017894	49581415	49581657
ENSE00001129677	49583556	49583774
ENSE00001129683	49582362	49582482
ENSE00001146777	49586746	49586850
ENSE00001190878	49569437	49569548
ENSE00001190884	49567442	49567621
ENSE00001236948	49590501	49599185
ENSE00001236965	49575369	49575590
ENSE00002696074	49562057	49562405
ENSE00003506085	49565317	49565498

Expression profiles

Bgee: expression breadth ubiquitous, 195 present calls, max score 99.26.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 12.0177 / max 341.2451, expressed in 1113 samples.

Highest expression (Bgee): ventricular zone, lobe of thyroid gland, thyroid gland, lobe of liver, ganglionic eminence.

Genetic regulation across tissues (GTEx eQTL / sQTL)

LIPG is an eGene in GTEx v10 — its expression is genetically regulated (eQTL) in 23 tissues and its splicing (sQTL) in 1 (q < 0.05). Strongest associations first; slope = normalized effect of the lead variant’s alternative allele.

showing 20 of 24 significant tissue × QTL associations:

Tissue	QTL	q-value	Slope	Lead variant
Muscle Skeletal	eqtl	1.4e-38	-0.48	18:49654294:A:G
Thyroid	eqtl	2.6e-26	-0.49	18:49673511:A:T
Thyroid	sqtl	1.1e-19	+0.59	18:49567494:C:T
Cells Cultured fibroblasts	eqtl	1.4e-13	-0.37	18:49610657:T:C
Skin Sun Exposed Lower leg	eqtl	3.4e-10	+0.33	18:49638347:A:G
Stomach	eqtl	1.0e-08	-0.33	18:49647298:G:C
Skin Not Sun Exposed Suprapubic	eqtl	5.6e-06	+0.24	18:49568052:T:C
Esophagus Muscularis	eqtl	1.2e-05	+0.21	18:49727639:A:G
Pancreas	eqtl	4.8e-05	+0.40	18:49654333:G:A
Adipose Subcutaneous	eqtl	7.5e-05	+0.28	18:49665924:C:A
Nerve Tibial	eqtl	1.6e-04	+0.33	18:49664465:A:G
Breast Mammary Tissue	eqtl	1.8e-03	+0.18	18:49910648:A:G
Lung	eqtl	2.3e-03	+0.15	18:49742135:G:A
Esophagus Gastroesophageal Junction	eqtl	1.0e-02	-0.22	18:49656027:GTTAATGAGTGAA:G
Artery Coronary	eqtl	1.1e-02	+0.43	18:49895558:TC:T
Artery Aorta	eqtl	1.6e-02	-0.18	18:49571119:C:T
Brain Caudate basal ganglia	eqtl	1.7e-02	+0.26	18:49868561:C:G
Colon Sigmoid	eqtl	2.2e-02	-0.18	18:49648010:A:G
Adipose Visceral Omentum	eqtl	2.3e-02	+0.13	18:49726849:G:C
Colon Transverse	eqtl	2.6e-02	-0.10	18:49743116:A:G

FANTOM5 promoters

8 alternative TSS:

Promoter ID	TPM avg	Samples expressed
170239	11.5725	1094
170234	0.1520	54
170237	0.1214	42
170232	0.0479	19
170233	0.0424	15
170236	0.0416	10
170238	0.0213	1
170235	0.0185	7

Top tissues by expression

showing 100 of 277 tissues by Bgee expression score (0-100, higher = more expressed):

Tissue	Anatomy ID	Expression score	Quality
ventricular zone	UBERON:0003053	99.26	gold quality
right lobe of thyroid gland	UBERON:0001119	99.04	gold quality
left lobe of thyroid gland	UBERON:0001120	98.49	gold quality
thyroid gland	UBERON:0002046	98.28	gold quality
right lobe of liver	UBERON:0001114	94.65	gold quality
ganglionic eminence	UBERON:0004023	94.64	gold quality
pigmented layer of retina	UBERON:0001782	93.43	gold quality
retina	UBERON:0000966	93.40	gold quality
placenta	UBERON:0001987	92.09	gold quality
secondary oocyte	CL:0000655	90.98	gold quality
seminal vesicle	UBERON:0000998	90.66	gold quality
liver	UBERON:0002107	89.98	gold quality
oocyte	CL:0000023	87.76	gold quality
metanephros cortex	UBERON:0010533	87.26	gold quality
embryo	UBERON:0000922	85.69	gold quality
gall bladder	UBERON:0002110	84.81	gold quality
vermiform appendix	UBERON:0001154	83.51	gold quality
buccal mucosa cell	CL:0002336	82.64	silver quality
islet of Langerhans	UBERON:0000006	82.30	gold quality
rectum	UBERON:0001052	81.04	gold quality
caecum	UBERON:0001153	78.99	gold quality
cartilage tissue	UBERON:0002418	78.20	gold quality
cortical plate	UBERON:0005343	76.54	gold quality
smooth muscle tissue	UBERON:0001135	76.17	gold quality
ileal mucosa	UBERON:0000331	75.58	gold quality
mucosa of transverse colon	UBERON:0004991	75.04	gold quality
upper lobe of left lung	UBERON:0008952	74.73	gold quality
small intestine Peyer’s patch	UBERON:0003454	74.65	gold quality
colonic epithelium	UBERON:0000397	74.64	gold quality
upper lobe of lung	UBERON:0008948	74.36	gold quality
small intestine	UBERON:0002108	74.22	gold quality
mucosa of sigmoid colon	UBERON:0004993	74.14	gold quality
adult mammalian kidney	UBERON:0000082	73.94	gold quality
testis	UBERON:0000473	73.37	gold quality
transverse colon	UBERON:0001157	73.36	gold quality
left testis	UBERON:0004533	73.12	gold quality
male germ line stem cell (sensu Vertebrata) in testis	CL:0000089 ∩ UBERON:0000473	72.92	gold quality
right testis	UBERON:0004534	72.68	gold quality
primordial germ cell in gonad	CL:0000670 ∩ UBERON:0000991	72.04	silver quality
duodenum	UBERON:0002114	71.79	gold quality
jejunal mucosa	UBERON:0000399	71.76	gold quality
colonic mucosa	UBERON:0000317	71.68	gold quality
intestine	UBERON:0000160	71.45	gold quality
cauda epididymis	UBERON:0004360	70.65	gold quality
large intestine	UBERON:0000059	70.31	gold quality
colon	UBERON:0001155	70.31	gold quality
pancreas	UBERON:0001264	69.57	gold quality
right hemisphere of cerebellum	UBERON:0014890	69.19	gold quality
kidney	UBERON:0002113	69.18	gold quality
cerebellar cortex	UBERON:0002129	68.54	gold quality
cerebellar hemisphere	UBERON:0002245	68.47	gold quality
endometrium	UBERON:0001295	68.40	gold quality
cerebellum	UBERON:0002037	67.97	gold quality
C1 segment of cervical spinal cord	UBERON:0006469	67.64	gold quality
metanephros	UBERON:0000081	67.61	gold quality
gastrocnemius	UBERON:0001388	67.49	gold quality
lung	UBERON:0002048	67.44	gold quality
mucosa of urinary bladder	UBERON:0001259	67.39	silver quality
corpus epididymis	UBERON:0004359	66.10	silver quality
lymph node	UBERON:0000029	65.92	gold quality
spinal cord	UBERON:0002240	65.86	gold quality
muscle of leg	UBERON:0001383	65.33	gold quality
skin of abdomen	UBERON:0001416	65.25	gold quality
caput epididymis	UBERON:0004358	64.97	gold quality
tibialis anterior	UBERON:0001385	64.41	silver quality
muscle layer of sigmoid colon	UBERON:0035805	63.88	gold quality
cortex of kidney	UBERON:0001225	63.85	gold quality
body of stomach	UBERON:0001161	63.82	gold quality
stomach	UBERON:0000945	63.56	gold quality
olfactory segment of nasal mucosa	UBERON:0005386	63.02	gold quality
omental fat pad	UBERON:0010414	62.76	gold quality
body of pancreas	UBERON:0001150	62.74	gold quality
peritoneum	UBERON:0002358	62.70	gold quality
skin of leg	UBERON:0001511	62.57	gold quality
esophagus mucosa	UBERON:0002469	62.32	gold quality
visceral pleura	UBERON:0002401	61.95	silver quality
adipose tissue of abdominal region	UBERON:0007808	61.55	gold quality
zone of skin	UBERON:0000014	61.39	gold quality
descending thoracic aorta	UBERON:0002345	61.33	gold quality
muscle organ	UBERON:0001630	61.31	gold quality
skeletal muscle organ	UBERON:0014892	61.31	gold quality
amniotic fluid	UBERON:0000173	61.17	silver quality
upper leg skin	UBERON:0004262	60.96	gold quality
prostate gland	UBERON:0002367	60.84	gold quality
hypothalamus	UBERON:0001898	60.83	gold quality
decidua	UBERON:0002450	60.78	silver quality
right coronary artery	UBERON:0001625	60.45	gold quality
pancreatic ductal cell	CL:0002079	60.19	silver quality
left coronary artery	UBERON:0001626	59.59	gold quality
anatomical system	UBERON:0000467	59.46	gold quality
material anatomical entity	UBERON:0000465	59.23	gold quality
multicellular organism	UBERON:0000468	59.23	gold quality
urinary bladder	UBERON:0001255	59.20	gold quality
esophagus	UBERON:0001043	59.07	gold quality
dorsal root ganglion	UBERON:0000044	58.69	silver quality
female reproductive system	UBERON:0000474	58.67	gold quality
uterus	UBERON:0000995	58.62	gold quality
coronary artery	UBERON:0001621	58.60	gold quality
lower lobe of lung	UBERON:0008949	58.51	silver quality
esophagogastric junction muscularis propria	UBERON:0035841	58.48	gold quality

Single-cell (SCXA)

Detected in 2 experiment(s), a significant marker in 1.

Experiment	Marker?	Max mean expression
E-GEOD-99795	no	5.92
E-ANND-3	no	0.00

HPA expression

RNA tissue specificity: Group enriched

showing 60 of 76 HPA tissues / cells by nTPM:

Tissue / cell	Axis	nTPM	Protein (IHC)
Thyroid gland	tissue	226.7	not detected
Placenta	tissue	140.4	not detected
Liver	tissue	32.5	not detected
Seminal vesicle	tissue	19.7	not detected
Appendix	tissue	15.4	not detected
Urinary bladder	tissue	13.4	not detected
Gallbladder	tissue	13.1	not detected
Hippocampus	tissue	7.9	not detected
Smooth muscle	tissue	7.2	not detected
Rectum	tissue	6.8	not detected
Small intestine	tissue	6.8	not detected
Testis	tissue	6.5	not detected
Duodenum	tissue	6.1	not detected
Choroid plexus	tissue	5.9
Colon	tissue	5.5	not detected
Spinal cord	tissue	4.9
Locus coeruleus	tissue	4.8
Retina	tissue	4.6
Adipose tissue	tissue	4.3	not detected
Kidney	tissue	4.2	not detected
Olfactory bulb	tissue	4.1
Cerebellum	tissue	3.9	not detected
Cerebral cortex	tissue	3.6	not detected
Insular cortex	tissue	3.6
Hippocampal formation	tissue	3.3
Entorhinal cortex	tissue	3.3
Retrosplenial cortex	tissue	3.3
Prefrontal cortex	tissue	3.2
Occipital cortex	tissue	3.2
Amygdala	tissue	3.1
Retrosplenial and cingulate cortex	tissue	3.1
Motor cortex	tissue	3.0
Periaqueductal gray	tissue	3.0
Somatosensory cortex	tissue	3.0
Temporal cortex	tissue	3.0
Frontal cortex	tissue	2.9
Basal ganglia	tissue	2.8	not detected
Corpus callosum	tissue	2.8
Ventral forebrain	tissue	2.8
Epididymis	tissue	2.7	not detected
Medulla oblongata	tissue	2.6
Septum	tissue	2.6
Postcentral gyrus	tissue	2.5
Putamen	tissue	2.4
Midbrain	tissue	2.4
Hypothalamus	tissue	2.4
Nucleus accumbens	tissue	2.3
Thalamus	tissue	2.3
Substantia nigra	tissue	2.3
Pons	tissue	2.2
Superior colliculi	tissue	1.9
Pancreas	tissue	1.8	not detected
Thymus	tissue	1.8
Lymph node	tissue	1.7	not detected
Tonsil	tissue	1.6	not detected
Lung	tissue	1.5	not detected
Prostate	tissue	1.4	not detected
Endometrium 1	tissue	1.3	not detected
Stomach 1	tissue	1.2	not detected
Ovary	tissue	1.1	not detected

Brain sub-regions (HPA Brain Atlas): detected in 189; highest nTPM — Cerebellar cortex (11.0), Habenula (10.6), Flocculonodular lobe (9.1), Hippocampus, CA1 (9.0), Nucleus tractus solitarii (8.8).

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): GTF3A, NFKB, NR1H3

miRNA regulators (miRDB)

Targeting LIPG by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific).

showing 30 of 97 miRNAs:

miRNA	Max score	Avg score	miRNA target_count
HSA-LET-7A-3P	100.00	74.03	3932
HSA-LET-7B-3P	100.00	74.08	3913
HSA-LET-7F-1-3P	100.00	74.02	3928
HSA-MIR-98-3P	100.00	74.08	3907
HSA-MIR-3924	100.00	72.09	2394
HSA-MIR-190A-3P	100.00	80.35	5520
HSA-MIR-4795-3P	100.00	74.62	4024
HSA-MIR-3662	99.99	73.82	5684
HSA-MIR-4775	99.98	75.00	6394
HSA-MIR-23B-5P	99.98	66.07	587
HSA-MIR-4789-5P	99.98	70.76	2721
HSA-MIR-568	99.98	69.86	2084
HSA-MIR-590-3P	99.96	74.34	6478
HSA-MIR-4666A-3P	99.96	71.71	3434
HSA-MIR-548AJ-3P	99.96	73.38	5345
HSA-MIR-548X-3P	99.96	73.38	5345
HSA-MIR-559	99.95	72.28	3609
HSA-MIR-548AB	99.95	71.31	3488
HSA-MIR-23A-5P	99.94	65.39	468
HSA-MIR-548A-5P	99.94	71.27	3482
HSA-MIR-548AD-5P	99.94	71.23	3502
HSA-MIR-548AE-5P	99.94	71.23	3502
HSA-MIR-548AK	99.94	71.24	3488
HSA-MIR-548AM-5P	99.94	71.24	3488
HSA-MIR-548AP-5P	99.94	71.14	3489
HSA-MIR-548AQ-5P	99.94	71.34	3426
HSA-MIR-548AR-5P	99.94	71.28	3515
HSA-MIR-548AS-5P	99.94	71.22	3482
HSA-MIR-548AU-5P	99.94	71.24	3488
HSA-MIR-548AY-5P	99.94	71.23	3502

Functional genomics

gnomAD constraint: pLI 1.54e-08, LOEUF 0.883, missense Z 1.44 — population loss-of-function intolerance (pLI ≥ 0.9 = LoF-intolerant; lower LOEUF = more constrained). gnomAD

Regional missense constraint (gnomAD RMC): no regional variation along ENST00000261292 — one region, missense o/e 0.89.

Literature-anchored findings (GeneRIF, showing 40)

• EDL mediates both HDL binding and uptake, and the selective uptake of HDL-CE, independently of lipolysis and CLA-1. (PMID:12164779)
• Endothelial lipase has a role in HDL metabolism [review] (PMID:12569156)
• EL is a major determinant of HDL concentration in humans (PMID:12601178)
• Expression of human endothelial lipase in mice results in dose-dependent increase in postheparin plasma phospholipase activity, catabolic rate of HDL-apolipoprotein, and uptake of apoA-I in both kidney and liver (PMID:14517167)
• Hepatic expression of human EL in mice resulted in markedly decreased levels of VLDL/LDL cholesterol, phospholipid, and apoB accompanied by significantly increased LDL apolipoprotein and phospholipid catabolism. (PMID:15117821)
• N-linked glycosylation has a role in the secretion and activity of endothelial lipase (PMID:15342690)
• results suggest that endothelial lipase (EL) on the endothelial cell surface can promote monocyte adhesion to the vascular endothelium through the interaction with heparan sulfate proteoglycans (PMID:15485805)
• The Endothelial lipase (EL) is a recently discovered member of the triglyceride-lipase family that is involved in plasma HDL metabolism. (PMID:15576837)
• LIPG variants are associated with HDL related risk factors, and may play a role in susceptibility to cardiovascular disease in this population. (PMID:16023652)
• regulatory elements in 11.4 kb of 5’ and 9.9 kb of 3’ region express in small intestine, ovary, testis, mammary gland, brain, lung, aorta, adipose tissue and adrenals; those between 27.4 and 11.4 kb of 5’ or 9.9 and 48.7 kb of 3’ region in kidney (PMID:16039280)
• the presence of apoA-II on HDL particles inhibits the ability of endothelial lipase to influence the metabolism of HDL in vivo (PMID:16877778)
• maternal type 1 diabetes is associated with TG accumulation and increased EL and HSL gene expression in placenta (PMID:16940551)
• strong association between proinflammatory cytokines and plasma EL concentrations among healthy people with low or high visceral adipose tissue (VAT) levels (PMID:16980590)
• suppression of either LPL or EL decreases proinflammatory cytokine expression and influences the lipid composition of THP-1 macrophages. (PMID:17093291)
• N-linked glycosylation at Asn-116 reduces the ability of EL to hydrolyze lipids in LDL and HDL2 (PMID:17322565)
• EL is the predominant TLG family member in the human placenta present at both interfaces; EL and LPL are dysregulated in growth restricted pregnancy (PMID:17356047)
• endothelial lipase plays a role in the etiology of the atherogenic plasma lipoprotein profile characteristic of the metabolic syndrome [review] (PMID:17495604)
• The 584C/T polymorphism of the EL gene was associated with AMI independently of HDL-C levels and thus may be involved in the pathogenesis of acute myocardial infarction (PMID:17526978)
• phospholipase activities of EL N118A, EL N375A, & EL N473A were significantly diminished relative to that of wild-type EL, with greatest reduction being apparent for (E3)rHDL. activity of EL N62A was increased up to 6X relative to that of wild-type EL (PMID:17545692)
• macrophages in advanced atherosclerotic lesions display high levels of endothelial lipase (EL) expression and the level of EL expression varies greatly during transformation of blood monocytes into foam cells (PMID:17570372)
• atorvastatin reduces LPL and EL expression by reducing the activation of LXRalpha and NF-kappaB, respectively (PMID:17644777)
• adiponectin is a significant metabolic concomitant of HTGL activity in African Americans (PMID:17651673)
• Endothelial lipase expression promotes the binding and uptake of native and oxidized LDL in THP-1 macrophages in a heparan sulfate proteoglycan-dependent manner. (PMID:17822686)
• The endothelial lipase 584C/T allele at codon 111 is associated with protection from coronary artery disease in a Chinese population. (PMID:17986713)
• after stimulation, the protease activity of PC5A is enhanced, as evidenced by the cleavage of the PC5A substrates Lefty, ADAMTS-4, endothelial lipase, and PCSK9. (PMID:18039650)
• Endothelial lipase appears to promote apolipoprotein A-I-mediated cholesterol efflux through catalytic and noncatalytic-dependent mechanisms in maacrophages. (PMID:18988890)
• SR-BI-mediated selective uptake of HDL cholesteryl ester is essential for the remodeling of large alpha-migrating HDL particles by EL. (PMID:19136670)
• the low-frequency Asn396Ser variant is significantly associated with increased HDL-C, while the common Thr111Ile variant is not (PMID:19287092)
• significant gene-physical inactivity interaction for HDL & some LDL measures for LIPG i24582 polymorphism. Higher levels of physical activity may be protective for HDL-C concentrations & low activity detrimental in LIPG i24582 TT women. (PMID:19380136)
• analysis among healthy Caucasian men and women from three independent studies does not support an association between the T111I variant and HDL-C, other plasma lipids, or risk of Coronary Heart Disease. (PMID:19411665)
• Thus, this N-terminal variant results in reduced secretion of endothelial lipase, plausibly leading to increased HDL-C levels. (PMID:19411705)
• The active form of EL is a homodimer in head-to-tail conformation. (PMID:19567873)
• LPL and LIPG are reported in the human testis and in germ cell neoplasms. (PMID:19780863)
• Statins can reduce EL expression in vitro and in vivo via inhibition of RhoA activity. The inhibition of EL expression in the vessel wall may contribute to the anti-atherogenic effects of statins. (PMID:20045866)
• common genetic variation in endothelial lipase (LIPG) does not appear to have a role in risk for coronary artery disease and deep venous thrombosis (PMID:20466371)
• It seems that plasma endothelial lipase levels in individuals with atherosclerosis might be higher than that measured in healthy individuals. [review] (PMID:20621031)
• Sulforaphane inhibits endothelial lipase expression via inhibition of NF-kappaB which may have a beneficial effect on HDL cholesterol levels (PMID:20688330)
• The LIPG 584T allele is associated with increased serum HDL-C, TC and ApoB levels. (PMID:20923576)
• Treatment of patients with coronary artery disease with lipid-modulation and/or antiplatelet drug may significantly decrease the expression of endothelial lipase. (PMID:21122200)
• Endothelial lipase and EL-generated lysophosphatidylcholines promote endothelial IL-8 synthesis. (PMID:21130993)

Cross-species orthologs

18 orthologs

Organism	Symbol	Gene ID
danio_rerio	lipg	ENSDARG00000031044
mus_musculus	Lipg	ENSMUSG00000053846
rattus_norvegicus	Lipg	ENSRNOG00000018694
drosophila_melanogaster	CG5162	FBGN0030828
drosophila_melanogaster	CG6675	FBGN0032973
drosophila_melanogaster	CG6472	FBGN0034166
drosophila_melanogaster	CG5665	FBGN0036977
drosophila_melanogaster	sxe2	FBGN0038398
drosophila_melanogaster	CG4582	FBGN0039344
drosophila_melanogaster	CG6296	FBGN0039470
drosophila_melanogaster	CG6295	FBGN0039471
drosophila_melanogaster	CG17192	FBGN0039472
drosophila_melanogaster	CG17191	FBGN0039473
drosophila_melanogaster	CG6283	FBGN0039474
drosophila_melanogaster	CG6277	FBGN0039475
drosophila_melanogaster	CG6271	FBGN0039476
drosophila_melanogaster	CG4267	FBGN0264979
drosophila_melanogaster	CG18258	FBGN0265267

Paralogs (9): PLA1A (ENSG00000144837), LIPH (ENSG00000163898), LIPC (ENSG00000166035), LPL (ENSG00000175445), PNLIP (ENSG00000175535), PNLIPRP1 (ENSG00000187021), LIPI (ENSG00000188992), PNLIPRP3 (ENSG00000203837), PNLIPRP2 (ENSG00000266200)

Mouse-model phenotypes

Observed phenotypes of the mouse ortholog (MGI:1341803) from MGI (Alliance of Genome Resources) — knockout/mutant phenotypes, ranked by annotation count. 7 distinct phenotype terms.

Mouse phenotype (MP)	Records
increased circulating HDL cholesterol level	3
increased circulating phospholipid level	3
increased circulating cholesterol level	3
increased circulating triglyceride level	2
abnormal circulating HDL cholesterol level	1
abnormal vascular endothelial cell physiology	1
abnormal cholesterol homeostasis	1

Additional cross-species homologs

Sequence homologs in species beyond Ensembl Compara’s model organisms, by Diamond local protein alignment (% sequence identity; best hit per species). Lower-identity rows are more distant homologs. The matched accessions’ gene symbols aren’t in biobtree yet, so each row shows the UniProt accession.

Organism	UniProt	Identity	Method
Vespa basalis	A0A0M3KKW3	100.0%	Diamond
Vespa affinis	P0DMB4	100.0%	Diamond
Polistes dominula	Q6Q251	99.7%	Diamond
Bos taurus	P11151	99.4%	Diamond
Papio anubis	P49060	99.4%	Diamond
Ovis aries	Q29524	99.4%	Diamond
Pongo abelii	Q5RBQ5	98.2%	Diamond
Neogale vison	O46647	96.2%	Diamond
Felis catus	P55031	96.2%	Diamond
Vespa velutina	C0HLL3	95.7%	Diamond
Vespula vulgaris	P49369	95.0%	Diamond
Vespula maculifrons	P51528	95.0%	Diamond
Vespula germanica	Q3ZU95	94.7%	Diamond
Sus scrofa	P49923	92.9%	Diamond
Vespa tropica	P0DPT0	92.4%	Diamond
Vespa crabro	P0CH87	92.0%	Diamond
Xenopus tropicalis	Q5XGE9	92.0%	Diamond
Xenopus laevis	Q6PA23	92.0%	Diamond
Vespa magnifica	P0CH47	91.4%	Diamond
Cavia porcellus	P11153	88.3%	Diamond
Ictidomys tridecemlineatus	O88354	85.8%	Diamond
Canis lupus familiaris	P06857	85.2%	Diamond
Polistes annularis	Q9U6W0	84.7%	Diamond
Equus caballus	P29183	83.6%	Diamond
Myocastor coypus	Q64425	82.3%	Diamond
Oryctolagus cuniculus	Q9BDJ4	82.3%	Diamond
Polybia paulista	A2VBC4	81.1%	Diamond
Dolichovespula maculata	P53357	80.9%	Diamond
Gallus gallus	P11602	77.4%	Diamond
Crotalus adamanteus	J3RZ81	68.4%	Diamond
Vespula squamosa	P0CH86	68.4%	Diamond
Ceratitis capitata	P27878	56.9%	Diamond
Dinoponera quadriceps	P0DSI2	38.6%	Diamond

Genomic neighbors (locus context)

Genes flanking this one on the chromosome (NCBI/Entrez gene neighborhood). Positional context only — some neighbors share regulatory elements (bidirectional promoters, antisense/overlapping transcripts), but chromosomal adjacency is not itself a functional relationship (see Interactions for that).

Symbol	Type	Entrez
LINC02837	ncRNA	101928144
SNHG22	ncRNA	103091864
ACAA2	protein-coding	10449
SCARNA17	ncRNA	677769
RPL17-C18orf32	protein-coding	100526842
SNORD58B	snoRNA	26790
SNORD58A	snoRNA	26791
RPL17	protein-coding	6139
MYO5B	protein-coding	4645

Protein

Protein identifiers

Endothelial lipase — Q9Y5X9 (reviewed: Q9Y5X9)

Alternative names: Endothelial cell-derived lipase, Phospholipase A1

All UniProt accessions (5): A0A075B751, B4DTR8, Q9Y5X9, J3KTN7, J3QQQ0

UniProt curated annotations — full annotation on UniProt →

Function. Exerts both phospholipase and triglyceride lipase activities. More active as a phospholipase than a triglyceride lipase. Hydrolyzes triglycerides, both with short-chain fatty acyl groups (tributyrin) and long-chain fatty acyl groups (triolein) with similar levels of activity toward both types of substrates. Hydrolyzes high density lipoproteins (HDL) more efficiently than other lipoproteins.

Subunit / interactions. Head to tail homodimer.

Subcellular location. Secreted.

Tissue specificity. High level of expression in the liver, placenta, lung, thyroid, kidney, testis and in the corpus luteum of the ovary. Expressed also in coronary artery endothelial cells, umbilical vein endothelial cells and in hepatocytes and osteosarcoma cell lines. Not detected in heart, brain and muscle.

Activity regulation. Inhibited by serum and NaCl.

Miscellaneous. It is termed endothelial lipase due to the fact that it is synthesized in endothelial cells, a characteristic that distinguishes it from other members of the family. However, this protein is also expressed in other cell types.

Similarity. Belongs to the AB hydrolase superfamily. Lipase family.

Isoforms (2)

UniProt ID	Names	Canonical?
Q9Y5X9-1	1	yes
Q9Y5X9-2	2

RefSeq proteins (2): NP_001294935, NP_006024* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000734	TAG_lipase	Family
IPR001024	PLAT/LH2_dom	Domain
IPR002330	Lipo_Lipase	Family
IPR013818	Lipase	Domain
IPR016272	Lipase_LIPH	Family
IPR029058	AB_hydrolase_fold	Homologous_superfamily
IPR033906	Lipase_N	Domain
IPR036392	PLAT/LH2_dom_sf	Homologous_superfamily

Pfam: PF00151, PF01477

Catalyzed reactions (Rhea)

• a triacylglycerol + H2O = a diacylglycerol + a fatty acid + H(+) (RHEA:12044)
• a 1,2-diacyl-sn-glycero-3-phosphocholine + H2O = a 2-acyl-sn-glycero-3-phosphocholine + a fatty acid + H(+) (RHEA:18689)
• 1,2,3-tri-(9Z-octadecenoyl)-glycerol + H2O = di-(9Z)-octadecenoylglycerol + (9Z)-octadecenoate + H(+) (RHEA:38575)
• 1,2,3-tributanoylglycerol + H2O = dibutanoylglycerol + butanoate + H(+) (RHEA:40475)
• 1,2-dihexadecanoyl-sn-glycero-3-phosphocholine + H2O = hexadecanoyl-sn-glycero-3-phosphocholine + hexadecanoate + H(+) (RHEA:41384)

UniProt features (24 total): glycosylation site 5, disulfide bond 5, sequence variant 4, active site 3, splice variant 2, signal peptide 1, chain 1, domain 1, sequence conflict 1, binding site 1

Structure

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q9Y5X9-F1	82.76	0.64

Human Protein Atlas

Protein class: Enzymes, ENZYME proteins, Hydrolases, Metabolic proteins, Predicted secreted proteins, Predicted intracellular proteins, Plasma proteins

Protein evidence: Evidence at protein level

Antibody reliability (HPA): IH uncertain

Functional residue map

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

Catalytic / active sites (3)

Position	Role
169	nucleophile
193	charge relay system
274	charge relay system

Ligand- & substrate-binding residues (1)

Position	Role
325–337	heparin

Disulfide bonds (5)

Type	Positions
Disulfide bond	64–77, 252–272, 297–316, 308–311, 463–483

Glycosylation sites (5)

Type	Positions
N-linked (glcnac…) asparagine	469, 491, 80, 136, 393

Function

Pathways and Gene Ontology

Reactome pathways

1 curated (TAS) of 4; 0 disease pathways. Curated-first; evidence = TAS (manually curated) vs IEA (electronic inference).

4 pathways:

ID	Pathway	Evidence
R-HSA-8964058	HDL remodeling	curated
R-HSA-174824	Plasma lipoprotein assembly, remodeling, and clearance	—
R-HSA-8963899	Plasma lipoprotein remodeling	—
R-HSA-382551	Transport of small molecules	—

MSigDB gene sets: 228 (showing top): GOBP_PHOSPHOLIPID_METABOLIC_PROCESS, GOBP_STEROL_HOMEOSTASIS, GOBP_LIPOPROTEIN_METABOLIC_PROCESS, GOCC_CELL_SURFACE, MCBRYAN_PUBERTAL_TGFB1_TARGETS_UP, GOBP_POSITIVE_REGULATION_OF_STEROL_TRANSPORT, GOBP_ORGANOPHOSPHATE_METABOLIC_PROCESS, GOBP_MONOCARBOXYLIC_ACID_METABOLIC_PROCESS, BILD_SRC_ONCOGENIC_SIGNATURE, GOBP_ORGANIC_ACID_BIOSYNTHETIC_PROCESS, GOBP_POSITIVE_REGULATION_OF_LIPID_TRANSPORT, SHEPARD_BMYB_MORPHOLINO_DN, GOBP_ORGANIC_HYDROXY_COMPOUND_TRANSPORT, GOBP_LIPID_HOMEOSTASIS, GOBP_GLYCEROLIPID_METABOLIC_PROCESS

GO Biological Process (12): lipid metabolic process (GO:0006629), fatty acid biosynthetic process (GO:0006633), response to nutrient (GO:0007584), phospholipid catabolic process (GO:0009395), positive regulation of high-density lipoprotein particle clearance (GO:0010983), triglyceride catabolic process (GO:0019433), positive regulation of cholesterol transport (GO:0032376), high-density lipoprotein particle remodeling (GO:0034375), cholesterol homeostasis (GO:0042632), reverse cholesterol transport (GO:0043691), phospholipid homeostasis (GO:0055091), lipid catabolic process (GO:0016042)

GO Molecular Function (9): lipoprotein lipase activity (GO:0004465), glycerophospholipase activity (GO:0004620), triacylglycerol lipase activity (GO:0004806), heparin binding (GO:0008201), glycerophospholipid phospholipase A1 activity (GO:0008970), protein binding (GO:0005515), lipase activity (GO:0016298), hydrolase activity (GO:0016787), carboxylic ester hydrolase activity (GO:0052689)

GO Cellular Component (4): extracellular region (GO:0005576), early endosome (GO:0005769), Golgi apparatus (GO:0005794), cell surface (GO:0009986)

Reactome top-level categories

3 top-level categories:

Category	Pathways
Plasma lipoprotein remodeling	1
Transport of small molecules	1
Plasma lipoprotein assembly, remodeling, and clearance	1

GO top-level categories

37 GO namespaces:

Category	Terms
cholesterol transport	2
hydrolase activity, acting on ester bonds	2
cellular anatomical structure	2
primary metabolic process	1
fatty acid metabolic process	1
lipid biosynthetic process	1
monocarboxylic acid biosynthetic process	1
response to nutrient levels	1
response to chemical	1
phospholipid metabolic process	1
lipid catabolic process	1
organophosphate catabolic process	1
regulation of high-density lipoprotein particle clearance	1
positive regulation of lipoprotein particle clearance	1
high-density lipoprotein particle clearance	1
triglyceride metabolic process	1
acylglycerol catabolic process	1
positive regulation of sterol transport	1
regulation of cholesterol transport	1
plasma lipoprotein particle remodeling	1
sterol homeostasis	1
lipid homeostasis	1
lipid metabolic process	1
catabolic process	1
triacylglycerol lipase activity	1
phospholipase activity	1
lipase activity	1
carboxylic ester hydrolase activity	1
glycosaminoglycan binding	1
sulfur compound binding	1
A1-type glycerophospholipase activity	1
binding	1
catalytic activity	1
endosome	1
cytoplasm	1
endomembrane system	1
intracellular membrane-bounded organelle	1

Experimentally-supported GO annotations

GO terms backed by direct experimental evidence (ECO experimental codes) — 12 of 26 annotations. The rest are phylogenetic / computational / electronic (IEA).

12 experimentally-supported GO terms:

GO term	NS	Evidence
cholesterol homeostasis	BP	mutant phenotype
high-density lipoprotein particle remodeling	BP	mutant phenotype
phospholipid homeostasis	BP	mutant phenotype
positive regulation of cholesterol transport	BP	direct assay
positive regulation of high-density lipoprotein particle clearance	BP	mutant phenotype
reverse cholesterol transport	BP	mutant phenotype
Golgi apparatus	CC	direct assay
cell surface	CC	direct assay
early endosome	CC	direct assay
glycerophospholipase activity	MF	direct assay
glycerophospholipid phospholipase A1 activity	MF	direct assay
triacylglycerol lipase activity	MF	direct assay

Protein interactions and networks

STRING

showing 16 of 814 interactions by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
LIPG	POU2F3	Q9UKI9	830
LIPG	APOA1	P02647	820
LIPG	ANGPTL3	Q9Y5C1	799
LIPG	CETP	P11597	740
LIPG	ANGPTL8	Q6UXH0	691
LIPG	APOB	P04114	657
LIPG	LCAT	P04180	656
LIPG	PLTP	P55058	654
LIPG	LPAR3	Q9UBY5	612
LIPG	LDLR	P01130	611
LIPG	APOC3	P02656	606
LIPG	ABCA1	O95477	606
LIPG	APOA5	Q6Q788	606
LIPG	GPIHBP1	Q8IV16	582
LIPG	PCSK9	Q8NBP7	579
LIPG	ANGPTL4	Q9BY76	579

IntAct

Human interaction partners of LIPG in IntAct, one row per partner (best MIscore; records = supporting IntAct interaction records).

3 partners by confidence:

Partner	Interaction type	MIscore	Records
NRP1	association	0.530	2
TOR1B	association	0.350	1
EXOSC5	physical association	0.000	1

BioGRID (82 interactions; top human partners by supporting records): ABHD14A (Affinity Capture-MS; 2 records), CANX (Affinity Capture-MS; 2 records), DNAJC13 (Affinity Capture-MS; 2 records), HLA-C (Affinity Capture-MS; 2 records), MAPK14 (Affinity Capture-MS; 2 records), NRP1 (Affinity Capture-MS; 2 records), PLS1 (Affinity Capture-MS; 2 records), PTPRS (Affinity Capture-MS; 2 records), TMED10 (Affinity Capture-MS; 2 records), TMED2 (Affinity Capture-MS; 2 records), TMED4 (Affinity Capture-MS; 2 records), TMED5 (Affinity Capture-MS; 2 records), TMED9 (Affinity Capture-MS; 2 records), TRMT1 (Affinity Capture-MS; 2 records), TUBB1 (Affinity Capture-MS; 2 records)

Disease & clinical

Genetic variants

Variant evidence for LIPG: 244 ClinVar records (0 pathogenic / likely pathogenic); 116 GWAS associations.

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	132
Likely benign	81
Benign	20

SpliceAI

Top 10 splice-impact sites by Δscore (adjacent positions with the same effect merged into one range; 31 predictions of 768):

Position(s)	Effect	Δscore	Sites
18:49565467	donor_gain	1.0000
18:49565499–49565500	donor_loss	1.0000	5
18:49567440–49567441	acceptor_loss	1.0000	5
18:49567622–49567623	donor_loss	1.0000	4
18:49569436	acceptor_loss	1.0000
18:49569549–49569550	donor_loss	1.0000	5
18:49575588	donor_gain	1.0000
18:49583554–49583555	acceptor_loss	1.0000	3
18:49583555	acceptor_gain	1.0000
18:49583775–49583776	donor_loss	1.0000	5

AlphaMissense

926 missense substitutions predicted likely pathogenic (of 3,333 scored), across 238 residues. Top 20 hotspot residues, ranked by the number of likely-pathogenic substitutions (of those reachable by a single-nucleotide change), then by mean score:

Residue	Likely-pathogenic substitutions	Mean am_pathogenicity	Max am_pathogenicity
D193	8	0.990	0.997
H274	8	0.986	0.992
H220	8	0.980	0.998
S169	8	0.978	0.996
D240	8	0.963	0.990
D212	8	0.935	0.962
F303	8	0.927	0.993
H173	8	0.922	0.980
D217	8	0.906	0.972
D283	8	0.887	0.968
H90	8	0.886	0.967
F462	8	0.841	0.979
H348	8	0.806	0.957
C252	7	0.994	0.998
C297	7	0.994	0.998
F199	7	0.992	0.997
C272	7	0.991	0.997
C308	7	0.990	0.995
C316	7	0.986	0.995
W92	7	0.983	0.996

HPA cancer prognostics

RNA cancer specificity: Cancer enriched (Thyroid Carcinoma)

Disease associations

OMIM: gene MIM:603684 | disease phenotypes:

GWAS associations

showing 30 of 116 associations:

Study	Trait	p-value
GCST010241_209	Apolipoprotein A1 levels	0.000000e+00
GCST010241_212	Apolipoprotein A1 levels	5e-304
GCST010242_122	HDL cholesterol levels	4e-269
GCST010242_123	HDL cholesterol levels	2e-245
GCST008084_140	HDL cholesterol levels x alcohol consumption (drinkers vs non-drinkers) interaction (2df)	2e-121
GCST008075_67	HDL cholesterol levels x alcohol consumption (regular vs non-regular drinkers) interaction (2df)	6e-106
GCST008084_6	HDL cholesterol levels x alcohol consumption (drinkers vs non-drinkers) interaction (2df)	5e-92
GCST008075_208	HDL cholesterol levels x alcohol consumption (regular vs non-regular drinkers) interaction (2df)	2e-79
GCST004232_67	HDL cholesterol levels	2e-74
GCST006611_157	HDL cholesterol	3e-73
GCST010002_366	Refractive error	4e-60
GCST008085_168	HDL cholesterol levels in current drinkers	2e-58
GCST006005_32	High density lipoprotein cholesterol levels	6e-51
GCST000755_29	HDL cholesterol	3e-49
GCST011348_34	High density lipoprotein cholesterol levels	3e-47
GCST008070_57	HDL cholesterol levels	1e-45
GCST002223_19	HDL cholesterol	1e-44
GCST008085_33	HDL cholesterol levels in current drinkers	2e-43
GCST006614_92	Total cholesterol levels	1e-39
GCST009367_75	HDL cholesterol levels x short total sleep time interaction (2df test)	2e-38
GCST002899_1	HDL cholesterol	8e-36
GCST009368_60	HDL cholesterol levels x long total sleep time interaction (2df test)	1e-32
GCST004235_26	Total cholesterol levels	2e-32
GCST008070_4	HDL cholesterol levels	6e-32
GCST009368_61	HDL cholesterol levels x long total sleep time interaction (2df test)	8e-32
GCST006034_4	Total cholesterol levels	5e-30
GCST011346_15	Total cholesterol levels	2e-29
GCST008084_108	HDL cholesterol levels x alcohol consumption (drinkers vs non-drinkers) interaction (2df)	2e-28
GCST007850_2	HDL cholesterol	5e-27
GCST008075_6	HDL cholesterol levels x alcohol consumption (regular vs non-regular drinkers) interaction (2df)	1e-26

EFO canonical traits (from GWAS)

16 canonical traits:

EFO ID	Trait name
EFO:0004612	high density lipoprotein cholesterol measurement
EFO:0004574	total cholesterol measurement
EFO:0004529	lipid measurement
EFO:0003940	physical activity
EFO:0004458	C-reactive protein measurement
EFO:0005658	response to selective serotonin reuptake inhibitor
EFO:0005325	response to angiotensin-converting enzyme inhibitor
EFO:0008589	esterified cholesterol measurement
EFO:0004614	apolipoprotein A 1 measurement
EFO:0006335	systolic blood pressure
EFO:0006527	smoking status measurement
EFO:0004611	low density lipoprotein cholesterol measurement
EFO:0004329	alcohol drinking
EFO:0000195	metabolic syndrome
EFO:0007874	gut microbiome measurement
EFO:0009188	Red cell distribution width

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL5080 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

Phase ≥1, by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 38,508 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

1 molecules by phase:

Molecule	Name	Phase	Patents
CHEMBL175247	ORLISTAT	4	38,508

PharmGKB: 1 entry (CPIC guideline: no)

GtoPdb / IUPHAR curated pharmacology

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

Target class: enzyme — Hydrolases & Lipases

Most potent curated ligand interactions (2 total), top 2:

Ligand	Action	Affinity	Parameter
GSK-264220A	Irreversible inhibition	8.9	pIC50
compound 12 [PMID: 31990537]	Inhibition	8.3	pIC50

Binding affinities (BindingDB)

1183 measured of 1385 human assays (1386 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
2-[6-[4-(methoxymethyl)phenyl]-1,3-benzothiazol-2-yl]-2-methylsulfonyl-N-(2-sulfamoylethyl)acetamide	IC50	0.5 nM	US-8987314: Amide, urea or sulfone amide linked benzothiazole inhibitors of endothelial lipase
2-methoxyethyl N-[4-[2-[1-methylsulfonyl-2-oxo-2-(2-sulfamoylethylamino)ethyl]-1,3-benzothiazol-6-yl]phenyl]carbamate	IC50	0.5 nM	US-8987314: Amide, urea or sulfone amide linked benzothiazole inhibitors of endothelial lipase
2-[5-(6-methoxy-3-pyridinyl)-1,3-benzothiazol-2-yl]-2-methylsulfonyl-N-(2-sulfamoylethyl)acetamide	IC50	0.5 nM	US-8987314: Amide, urea or sulfone amide linked benzothiazole inhibitors of endothelial lipase
2-[5-(2-methoxy-4-pyridinyl)-1,3-benzothiazol-2-yl]-2-methylsulfonyl-N-(2-sulfamoylethyl)acetamide	IC50	0.5 nM	US-8987314: Amide, urea or sulfone amide linked benzothiazole inhibitors of endothelial lipase
N-(2-methoxyethyl)-4-[2-[1-methylsulfonyl-2-oxo-2-(2-sulfamoylethylamino)ethyl]-1,3-benzothiazol-5-yl]benzamide	IC50	0.5 nM	US-8987314: Amide, urea or sulfone amide linked benzothiazole inhibitors of endothelial lipase
2-[6-(3-fluoro-2-oxo-1H-pyridin-4-yl)-1,3-benzothiazol-2-yl]-2-methylsulfonyl-N-(2-sulfamoylethyl)acetamide	IC50	0.5 nM	US-8987314: Amide, urea or sulfone amide linked benzothiazole inhibitors of endothelial lipase
N-cyclopropyl-4-[2-[2-oxo-2-(2-sulfamoylethylamino)-1-[[4-(trifluoromethoxy)phenyl]methylsulfonyl]ethyl]-1,3-benzothiazol-6-yl]benzamide	IC50	0.5 nM	US-8987314: Amide, urea or sulfone amide linked benzothiazole inhibitors of endothelial lipase
4-[2-[2-oxo-2-(2-sulfamoylethylamino)-1-[[4-(trifluoromethoxy)phenyl]methylsulfonyl]ethyl]-1,3-benzothiazol-6-yl]benzamide	IC50	0.5 nM	US-8987314: Amide, urea or sulfone amide linked benzothiazole inhibitors of endothelial lipase
2-[5-(6-fluoro-3-pyridinyl)-1,3-benzothiazol-2-yl]-N-(2-sulfamoylethyl)-2-[[4-(trifluoromethoxy)phenyl]methylsulfonyl]acetamide	IC50	0.5 nM	US-8987314: Amide, urea or sulfone amide linked benzothiazole inhibitors of endothelial lipase
2-[5-(3-acetamidophenyl)-1,3-benzothiazol-2-yl]-2-methylsulfonyl-N-(2-sulfamoylethyl)acetamide	IC50	0.5 nM	US-8987314: Amide, urea or sulfone amide linked benzothiazole inhibitors of endothelial lipase
CHEMBL4460663	IC50	0.5 nM
2-methylsulfonyl-2-[6-(3-phenoxyphenyl)-1,3-benzothiazol-2-yl]-N-(2-sulfamoylethyl)acetamide	IC50	0.6 nM	US-8987314: Amide, urea or sulfone amide linked benzothiazole inhibitors of endothelial lipase
2-[5-[4-(3,3-difluoroazetidine-1-carbonyl)phenyl]-1,3-benzothiazol-2-yl]-2-methylsulfonyl-N-(2-sulfamoylethyl)acetamide	IC50	0.6 nM	US-8987314: Amide, urea or sulfone amide linked benzothiazole inhibitors of endothelial lipase
N-(2-methoxyethyl)-4-[2-[2-oxo-2-(2-sulfamoylethylamino)-1-[[4-(trifluoromethoxy)phenyl]methylsulfonyl]ethyl]-1,3-benzothiazol-6-yl]benzamide	IC50	0.7 nM	US-8987314: Amide, urea or sulfone amide linked benzothiazole inhibitors of endothelial lipase
N-(3-hydroxypropyl)-4-[2-[1-methylsulfonyl-2-oxo-2-(2-sulfamoylethylamino)ethyl]-1,3-benzothiazol-6-yl]benzamide	IC50	0.7 nM	US-8987314: Amide, urea or sulfone amide linked benzothiazole inhibitors of endothelial lipase
4-[2-[1-(cyclopropylmethylsulfonyl)-2-oxo-2-(2-sulfamoylethylamino)ethyl]-1,3-benzothiazol-6-yl]-N-(2-methoxyethyl)-N-methylbenzamide	IC50	0.7 nM	US-8987314: Amide, urea or sulfone amide linked benzothiazole inhibitors of endothelial lipase
2-[6-[4-[(3S)-3-methoxypyrrolidine-1-carbonyl]phenyl]-1,3-benzothiazol-2-yl]-N-(2-sulfamoylethyl)-2-(3,3,3-trifluoropropylsulfonyl)acetamide	IC50	0.7 nM	US-8987314: Amide, urea or sulfone amide linked benzothiazole inhibitors of endothelial lipase
2-[6-[4-(3-fluoroazetidine-1-carbonyl)phenyl]-1,3-benzothiazol-2-yl]-2-methylsulfonyl-N-(2-sulfamoylethyl)acetamide	IC50	0.7 nM	US-8987314: Amide, urea or sulfone amide linked benzothiazole inhibitors of endothelial lipase
2-[5-[4-(methoxymethyl)phenyl]-1,3-benzothiazol-2-yl]-2-methylsulfonyl-N-(2-sulfamoylethyl)acetamide	IC50	0.7 nM	US-8987314: Amide, urea or sulfone amide linked benzothiazole inhibitors of endothelial lipase
2-[5-(2-fluoro-3-pyridinyl)-1,3-benzothiazol-2-yl]-2-methylsulfonyl-N-(2-sulfamoylethyl)acetamide	IC50	0.7 nM	US-8987314: Amide, urea or sulfone amide linked benzothiazole inhibitors of endothelial lipase
2-[6-(4-acetamidophenyl)-1,3-benzothiazol-2-yl]-N-(2-sulfamoylethyl)-2-(3,3,3-trifluoropropylsulfonyl)acetamide	IC50	0.8 nM	US-8987314: Amide, urea or sulfone amide linked benzothiazole inhibitors of endothelial lipase
4-[2-[1-(cyclopropylmethylsulfonyl)-2-oxo-2-(2-sulfamoylethylamino)ethyl]-1,3-benzothiazol-6-yl]-N-(2-methoxyethyl)benzamide	IC50	0.8 nM	US-8987314: Amide, urea or sulfone amide linked benzothiazole inhibitors of endothelial lipase
2-[6-(3-chlorophenyl)-1,3-benzothiazol-2-yl]-2-methylsulfonyl-N-(2-sulfamoylethyl)acetamide	IC50	0.8 nM	US-8987314: Amide, urea or sulfone amide linked benzothiazole inhibitors of endothelial lipase
N-(2-methoxyethyl)-N-methyl-4-[2-[2-oxo-2-(2-sulfamoylethylamino)-1-[[4-(trifluoromethyl)phenyl]methylsulfonyl]ethyl]-1,3-benzothiazol-6-yl]benzamide	IC50	0.8 nM	US-8987314: Amide, urea or sulfone amide linked benzothiazole inhibitors of endothelial lipase
2-[5-(2-fluorophenyl)-1,3-benzothiazol-2-yl]-2-methylsulfonyl-N-(2-sulfamoylethyl)acetamide	IC50	0.8 nM	US-8987314: Amide, urea or sulfone amide linked benzothiazole inhibitors of endothelial lipase
2-methylsulfonyl-2-(5-pyrimidin-2-yl-1,3-benzothiazol-2-yl)-N-(2-sulfamoylethyl)acetamide	IC50	0.8 nM	US-8987314: Amide, urea or sulfone amide linked benzothiazole inhibitors of endothelial lipase
4-[2-[1-(cyclopropylmethylsulfonyl)-2-oxo-2-(2-sulfamoylethylamino)ethyl]-1,3-benzothiazol-6-yl]-N-(2-methoxy-2-methylpropyl)benzamide	IC50	0.9 nM	US-8987314: Amide, urea or sulfone amide linked benzothiazole inhibitors of endothelial lipase
CHEMBL4563019	IC50	0.9 nM
2-methylsulfonyl-2-[5-(6-oxo-1H-pyridin-3-yl)-1,3-benzothiazol-2-yl]-N-(2-sulfamoylethyl)acetamide	IC50	1 nM	US-8987314: Amide, urea or sulfone amide linked benzothiazole inhibitors of endothelial lipase
2-[(4-fluorophenyl)methylsulfonyl]-2-[5-(6-fluoro-3-pyridinyl)-1,3-benzothiazol-2-yl]-N-(2-sulfamoylethyl)acetamide	IC50	1 nM	US-8987314: Amide, urea or sulfone amide linked benzothiazole inhibitors of endothelial lipase
N-(2-hydroxy-2-methylpropyl)-3-[2-[2-oxo-2-(2-sulfamoylethylamino)-1-(3,3,3-trifluoropropylsulfonyl)ethyl]-1,3-benzothiazol-6-yl]benzamide	IC50	1 nM	US-8987314: Amide, urea or sulfone amide linked benzothiazole inhibitors of endothelial lipase
2-benzylsulfonyl-2-[5-methyl-6-[4-(piperidine-1-carbonyl)phenyl]-1,3-benzothiazol-2-yl]-N-(2-sulfamoylethyl)acetamide	IC50	1 nM	US-8987314: Amide, urea or sulfone amide linked benzothiazole inhibitors of endothelial lipase
benzyl N-[4-[2-[2-[[2-(cyclopropylamino)-2-oxoethyl]amino]-1-methylsulfonyl-2-oxoethyl]-6-fluoro-1,3-benzothiazol-5-yl]phenyl]carbamate	IC50	1 nM	US-10173991: Sulfone amide linked benzothiazole inhibitors of endothelial lipase
benzyl N-[4-[2-[2-[[2-(cyclopropylamino)-2-oxoethyl]amino]-2-oxo-1-(3,3,3-trifluoropropylsulfonyl)ethyl]-6-fluoro-1,3-benzothiazol-5-yl]phenyl]carbamate	IC50	1 nM	US-10173991: Sulfone amide linked benzothiazole inhibitors of endothelial lipase
benzyl N-[4-[2-[2-[[2-(cyclopropylamino)-2-oxoethyl]amino]-1-(3-hydroxypropylsulfonyl)-2-oxoethyl]-6-fluoro-1,3-benzothiazol-5-yl]phenyl]carbamate	IC50	1 nM	US-10173991: Sulfone amide linked benzothiazole inhibitors of endothelial lipase
benzyl N-[4-[2-[2-[[2-(cyclopropylamino)-2-oxoethyl]amino]-1-cyclopropylsulfonyl-2-oxoethyl]-6-fluoro-1,3-benzothiazol-5-yl]phenyl]carbamate	IC50	1 nM	US-10173991: Sulfone amide linked benzothiazole inhibitors of endothelial lipase
benzyl N-[4-[2-[2-[[2-(cyclopropylamino)-2-oxoethyl]amino]-2-oxo-1-pentylsulfonylethyl]-5-fluoro-1,3-benzothiazol-6-yl]phenyl]carbamate	IC50	1 nM	US-10173991: Sulfone amide linked benzothiazole inhibitors of endothelial lipase
benzyl N-[4-[2-[2-[[2-(cyclopropylamino)-2-oxoethyl]amino]-2-oxo-1-propylsulfonylethyl]-5-fluoro-1,3-benzothiazol-6-yl]phenyl]carbamate	IC50	1 nM	US-10173991: Sulfone amide linked benzothiazole inhibitors of endothelial lipase
benzyl N-[4-[2-[1-(cyclohexylmethylsulfonyl)-2-[[2-(cyclopropylamino)-2-oxoethyl]amino]-2-oxoethyl]-5-fluoro-1,3-benzothiazol-6-yl]phenyl]carbamate	IC50	1 nM	US-10173991: Sulfone amide linked benzothiazole inhibitors of endothelial lipase
N-[2-(cyclopropylamino)-2-oxoethyl]-2-(3-hydroxypropylsulfonyl)-2-[6-[4-(1,3-oxazol-2-yl)phenyl]-1,3-benzothiazol-2-yl]acetamide	IC50	1 nM	US-10173991: Sulfone amide linked benzothiazole inhibitors of endothelial lipase
N-[2-(cyclopropylamino)-2-oxoethyl]-2-[5-fluoro-6-(3-pyrazol-1-ylphenyl)-1,3-benzothiazol-2-yl]-2-(3,3,3-trifluoropropylsulfonyl)acetamide	IC50	1 nM	US-10173991: Sulfone amide linked benzothiazole inhibitors of endothelial lipase
N-[2-(cyclopropylamino)-2-oxoethyl]-2-[5-fluoro-6-[4-(1H-pyrazol-5-yl)phenyl]-1,3-benzothiazol-2-yl]-2-(3,3,3-trifluoropropylsulfonyl)acetamide	IC50	1 nM	US-10173991: Sulfone amide linked benzothiazole inhibitors of endothelial lipase
N-[2-(cyclopropylamino)-2-oxoethyl]-2-[5-fluoro-6-(1-methylindazol-6-yl)-1,3-benzothiazol-2-yl]-2-methylsulfonylacetamide	IC50	1 nM	US-10173991: Sulfone amide linked benzothiazole inhibitors of endothelial lipase
N-[2-(cyclopropylamino)-2-oxoethyl]-2-[5-fluoro-6-(2-methyl-1,3-benzothiazol-5-yl)-1,3-benzothiazol-2-yl]-2-methylsulfonylacetamide	IC50	1 nM	US-10173991: Sulfone amide linked benzothiazole inhibitors of endothelial lipase
2-[6-(6-fluoro-3-pyridinyl)-1,3-benzothiazol-2-yl]-2-(2-methoxyethylsulfonyl)-N-[2-oxo-2-(2-phenylmethoxyethylamino)ethyl]acetamide	IC50	1 nM	US-10173991: Sulfone amide linked benzothiazole inhibitors of endothelial lipase
2-[6-(6-fluoro-3-pyridinyl)-1,3-benzothiazol-2-yl]-2-(2-methoxyethylsulfonyl)-N-[2-oxo-2-(2-phenoxyethylamino)ethyl]acetamide	IC50	1 nM	US-10173991: Sulfone amide linked benzothiazole inhibitors of endothelial lipase
benzyl N-{4-[2- ({[(cyclopropyl- carbamoyl)methyl] carbamoyl}[2- (morpholin-4-yl) ethanesulfonyl] methyl)-5-fluoro- 1,3-benzothiazol- 6-yl]phenyl} carbamate	IC50	1 nM	US-10173991: Sulfone amide linked benzothiazole inhibitors of endothelial lipase
N-[(cyclopropyl- carbamoyl) methyl]-2- (dimethyl- sulfamoyl)-2-[4- fluoro-6-(2- methyl-1-oxo-1,2- dihydro- isoquinolin-6-yl)- 1,3-benzothiazol- 2-yl]acetamide	IC50	1 nM	US-10173991: Sulfone amide linked benzothiazole inhibitors of endothelial lipase
2-(6-{4-[(benzyl- carbamoyl) amino]phenyl}- 5-fluoro-1,3- benzothiazol- 2-yl)-N- [(cyclopropyl- carbamoyl) methyl]-2-(3,3,3- trifluoropropane- sulfonyl)acetamide	IC50	1 nM	US-10173991: Sulfone amide linked benzothiazole inhibitors of endothelial lipase
(3-cyanophenyl) methyl N-{4-[2- ({[(cyclopropyl- carbamoyl) methyl] carbamoyl}(3,3,3- trifluoropropane- sulfonyl)methyl)- 5-fluoro-1,3- benzothiazol- 6-yl]phenyl} carbamate	IC50	1 nM	US-10173991: Sulfone amide linked benzothiazole inhibitors of endothelial lipase

ChEMBL bioactivities

1304 potent at pChembl≥5 of 1327 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
9.30	IC50	0.5	nM	CHEMBL3677434
9.30	IC50	0.5	nM	CHEMBL3682491
9.30	IC50	0.5	nM	CHEMBL3677556
9.30	IC50	0.5	nM	CHEMBL3672654
9.30	IC50	0.5	nM	CHEMBL3677634
9.30	IC50	0.5	nM	CHEMBL3677528
9.30	IC50	0.5	nM	CHEMBL3677557
9.30	IC50	0.5	nM	CHEMBL3677433
9.30	IC50	0.5	nM	CHEMBL3672653
9.30	IC50	0.5	nM	CHEMBL3677439
9.30	IC50	0.5	nM	CHEMBL4460663
9.22	IC50	0.6	nM	CHEMBL3677540
9.22	IC50	0.6	nM	CHEMBL3677646
9.15	IC50	0.7	nM	CHEMBL3677617
9.15	IC50	0.7	nM	CHEMBL3677457
9.15	IC50	0.7	nM	CHEMBL3682444
9.15	IC50	0.7	nM	CHEMBL3682490
9.15	IC50	0.7	nM	CHEMBL3677629
9.15	IC50	0.7	nM	CHEMBL3682495
9.15	IC50	0.7	nM	CHEMBL3677541
9.10	IC50	0.8	nM	CHEMBL3672645
9.10	IC50	0.8	nM	CHEMBL3677458
9.10	IC50	0.8	nM	CHEMBL3677538
9.10	IC50	0.8	nM	CHEMBL3677614
9.10	IC50	0.8	nM	CHEMBL3682486
9.10	IC50	0.8	nM	CHEMBL3682466
9.05	IC50	0.9	nM	CHEMBL3677572
9.05	IC50	0.9	nM	CHEMBL4563019
9.00	IC50	1	nM	CHEMBL3682462
9.00	IC50	1	nM	CHEMBL3682459
9.00	IC50	1	nM	CHEMBL3677530
9.00	IC50	1	nM	CHEMBL3677635
9.00	IC50	1	nM	CHEMBL4471611
9.00	IC50	1	nM	CHEMBL4460999
9.00	IC50	1	nM	CHEMBL5956748
9.00	IC50	1	nM	CHEMBL5828535
9.00	IC50	1	nM	CHEMBL5963511
9.00	IC50	1	nM	CHEMBL5943145
9.00	IC50	1	nM	CHEMBL6028347
9.00	IC50	1	nM	CHEMBL6035951
9.00	IC50	1	nM	CHEMBL6008474
9.00	IC50	1	nM	CHEMBL5748044
9.00	IC50	1	nM	CHEMBL5915088
9.00	IC50	1	nM	CHEMBL5822600
9.00	IC50	1	nM	CHEMBL5838092
9.00	IC50	1	nM	CHEMBL5792449
9.00	IC50	1	nM	CHEMBL5752680
9.00	IC50	1	nM	CHEMBL5925040
9.00	IC50	1	nM	CHEMBL5803110
9.00	IC50	1	nM	CHEMBL5741870

PubChem BioAssay actives

264 with measured affinity, of 348 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
4-[6-fluoro-2-[5-[(sulfamoylamino)methyl]-1,3,4-oxadiazole-2-carbonyl]-1,3-benzothiazol-5-yl]-N-(2,2,2-trifluoroethyl)benzamide	1529147: Inhibition of EL in human HT1080 cells using A10070 as substrate preincubated for 20 min followed by DMPG vesicle doped substrate addition and measured at 20 secs interval for 10 mins by fluorescence assay	ic50	0.0005	uM
2-[5-fluoro-6-(1-oxo-2,3-dihydroisoindol-5-yl)-1,3-benzothiazole-2-carbonyl]-5-[(sulfamoylamino)methyl]-1,3,4-oxadiazole	1529147: Inhibition of EL in human HT1080 cells using A10070 as substrate preincubated for 20 min followed by DMPG vesicle doped substrate addition and measured at 20 secs interval for 10 mins by fluorescence assay	ic50	0.0005	uM
5-fluoro-2-[5-[(sulfamoylamino)methyl]-1,3,4-oxadiazole-2-carbonyl]-N-(2,2,2-trifluoroethyl)-1,3-benzothiazole-6-carboxamide	1529147: Inhibition of EL in human HT1080 cells using A10070 as substrate preincubated for 20 min followed by DMPG vesicle doped substrate addition and measured at 20 secs interval for 10 mins by fluorescence assay	ic50	0.0005	uM
2-[6-fluoro-5-(1-oxo-2,3-dihydroisoindol-5-yl)-1,3-benzothiazole-2-carbonyl]-5-[(sulfamoylamino)methyl]-1,3,4-oxadiazole	1529147: Inhibition of EL in human HT1080 cells using A10070 as substrate preincubated for 20 min followed by DMPG vesicle doped substrate addition and measured at 20 secs interval for 10 mins by fluorescence assay	ic50	0.0005	uM
4-[2-fluoro-4-[5-fluoro-2-[5-[(sulfamoylamino)methyl]-1,3,4-oxadiazole-2-carbonyl]-1,3-benzothiazol-6-yl]benzoyl]morpholine	1529147: Inhibition of EL in human HT1080 cells using A10070 as substrate preincubated for 20 min followed by DMPG vesicle doped substrate addition and measured at 20 secs interval for 10 mins by fluorescence assay	ic50	0.0009	uM
benzyl N-[4-[2-[1-cyano-2-[[2-(cyclopropylamino)-2-oxoethyl]amino]-2-oxoethyl]-1,3-benzothiazol-6-yl]phenyl]carbamate	1601382: Inhibition of endothelial lipase (unknown origin)	ic50	0.0010	uM
2-[5-fluoro-6-(6-fluoro-3-pyridinyl)-1,3-benzothiazole-2-carbonyl]-5-[(sulfamoylamino)methyl]-1,3,4-oxadiazole	1529147: Inhibition of EL in human HT1080 cells using A10070 as substrate preincubated for 20 min followed by DMPG vesicle doped substrate addition and measured at 20 secs interval for 10 mins by fluorescence assay	ic50	0.0010	uM
1-benzyl-N-[3-(3,4-dichlorophenyl)propyl]-4-hydroxy-5-oxo-2H-pyrrole-3-carboxamide	1384994: Inhibition of endothelial lipase in human HT1080 cells using PED-A1 containing DMPG vesicles as substrate pretreated for 20 mins followed by substrate addition and measured every 20 secs for 10 mins by fluorescence assay	ic50	0.0036	uM
2-(3-phenylpropyl)-3-(trifluoromethyl)-1-azatricyclo[6.3.1.04,12]dodeca-2,4,6,8(12)-tetraen-6-amine	1056400: Inhibition of human endothelial lipase using PLAi as substrate measured for 30 mins by cell-based fluorescence assay	ic50	0.0040	uM
N-[2-(cyclopropylamino)-2-oxoethyl]-2-[6-(6-fluoro-3-pyridinyl)-1,3-benzothiazol-2-yl]-2-(2-methoxyethylsulfonyl)acetamide	1591499: Inhibition of human endothelial lipase derived from human HT1080 cell conditioned media using PED-A1 as substrate incubated for 20 mins and measured every 20 secs for 10 mins by FRET assay	ic50	0.0046	uM
2-[6-(6-fluoro-3-pyridinyl)-1,3-benzothiazol-2-yl]-2-methylsulfonyl-N-(2-sulfamoylethyl)acetamide	1591499: Inhibition of human endothelial lipase derived from human HT1080 cell conditioned media using PED-A1 as substrate incubated for 20 mins and measured every 20 secs for 10 mins by FRET assay	ic50	0.0050	uM
2-(6-phenyl-1,3-benzothiazole-2-carbonyl)-5-[(sulfamoylamino)methyl]-1,3,4-oxadiazole	1529147: Inhibition of EL in human HT1080 cells using A10070 as substrate preincubated for 20 min followed by DMPG vesicle doped substrate addition and measured at 20 secs interval for 10 mins by fluorescence assay	ic50	0.0050	uM
2-cyano-N-[2-(cyclopropylamino)-2-oxoethyl]-2-[6-(1-oxo-2,3-dihydroisoindol-5-yl)-1,3-benzothiazol-2-yl]acetamide	1601382: Inhibition of endothelial lipase (unknown origin)	ic50	0.0053	uM
N-[3-(3,4-dichlorophenyl)propyl]-4-hydroxy-5-oxo-1-(2-phenoxyethyl)-2H-pyrrole-3-carboxamide	1384994: Inhibition of endothelial lipase in human HT1080 cells using PED-A1 containing DMPG vesicles as substrate pretreated for 20 mins followed by substrate addition and measured every 20 secs for 10 mins by fluorescence assay	ic50	0.0054	uM
Orlistat	1586813: Inhibition of endothelial lipase in human HT1080 cells using PED-A1 containing DMPG vesicles as substrate pretreated for 20 mins followed by substrate addition and measured every 20 secs for 10 mins by fluorescence assay	ic50	0.0060	uM
2-[(6-phenyl-1,3-benzothiazol-2-yl)methyl]-5-[(sulfamoylamino)methyl]-1,3,4-oxadiazole	1586811: Inhibition of human endothelial lipase using HDL as substrate measured after 4 hrs	ic50	0.0060	uM
N-[2-(cyclopropylamino)-2-oxoethyl]-2-[6-(6-fluoro-3-pyridinyl)-1,3-benzothiazol-2-yl]-2-methylsulfonylacetamide	1591511: Inhibition of human endothelial lipase using D31-POPC-HDL as substrate incubated for 2 hrs in presence of human serum by LC/MS analysis	ic50	0.0070	uM
methyl N-[4-[2-[5-[(sulfamoylamino)methyl]-1,3,4-oxadiazole-2-carbonyl]-1,3-benzothiazol-6-yl]phenyl]carbamate	1529147: Inhibition of EL in human HT1080 cells using A10070 as substrate preincubated for 20 min followed by DMPG vesicle doped substrate addition and measured at 20 secs interval for 10 mins by fluorescence assay	ic50	0.0100	uM
5-[[5-[methylsulfonyl-[6-[4-(morpholine-4-carbonyl)phenyl]-1,3-benzothiazol-2-yl]methyl]-1,3,4-oxadiazol-2-yl]methyl]-1,3-thiazolidine-2,4-dione	1586813: Inhibition of endothelial lipase in human HT1080 cells using PED-A1 containing DMPG vesicles as substrate pretreated for 20 mins followed by substrate addition and measured every 20 secs for 10 mins by fluorescence assay	ic50	0.0100	uM
5-methyl-5-[[5-[methylsulfonyl-(6-phenyl-1,3-benzothiazol-2-yl)methyl]-1,3,4-oxadiazol-2-yl]methyl]imidazolidine-2,4-dione	1586813: Inhibition of endothelial lipase in human HT1080 cells using PED-A1 containing DMPG vesicles as substrate pretreated for 20 mins followed by substrate addition and measured every 20 secs for 10 mins by fluorescence assay	ic50	0.0100	uM
2-[6-(4-fluorophenyl)-1,3-benzothiazole-2-carbonyl]-5-[(sulfamoylamino)methyl]-1,3,4-oxadiazole	1529147: Inhibition of EL in human HT1080 cells using A10070 as substrate preincubated for 20 min followed by DMPG vesicle doped substrate addition and measured at 20 secs interval for 10 mins by fluorescence assay	ic50	0.0100	uM
N-[3-(3,4-dichlorophenyl)propyl]-1-ethyl-4-(methylamino)-5-oxo-2H-pyrrole-3-carboxamide	1384994: Inhibition of endothelial lipase in human HT1080 cells using PED-A1 containing DMPG vesicles as substrate pretreated for 20 mins followed by substrate addition and measured every 20 secs for 10 mins by fluorescence assay	ic50	0.0100	uM
2-[methylsulfonyl-(6-phenyl-1,3-benzothiazol-2-yl)methyl]-5-[(sulfamoylamino)methyl]-1,3,4-oxadiazole	1586813: Inhibition of endothelial lipase in human HT1080 cells using PED-A1 containing DMPG vesicles as substrate pretreated for 20 mins followed by substrate addition and measured every 20 secs for 10 mins by fluorescence assay	ic50	0.0100	uM
2-[benzylsulfonyl-(6-phenyl-1,3-benzothiazol-2-yl)methyl]-5-[(sulfamoylamino)methyl]-1,3,4-oxadiazole	1586813: Inhibition of endothelial lipase in human HT1080 cells using PED-A1 containing DMPG vesicles as substrate pretreated for 20 mins followed by substrate addition and measured every 20 secs for 10 mins by fluorescence assay	ic50	0.0100	uM
2-methylsulfonyl-2-[6-[1-(2-morpholin-4-ylethyl)pyrazol-4-yl]-1,3-benzothiazol-2-yl]-N-(2-sulfamoylethyl)acetamide	1591499: Inhibition of human endothelial lipase derived from human HT1080 cell conditioned media using PED-A1 as substrate incubated for 20 mins and measured every 20 secs for 10 mins by FRET assay	ic50	0.0100	uM
2-methylsulfonyl-2-(6-phenyl-1,3-benzothiazol-2-yl)-N-(2-sulfamoylethyl)acetamide	1591499: Inhibition of human endothelial lipase derived from human HT1080 cell conditioned media using PED-A1 as substrate incubated for 20 mins and measured every 20 secs for 10 mins by FRET assay	ic50	0.0100	uM
2-methylsulfonyl-2-[6-[4-(morpholine-4-carbonyl)phenyl]-1,3-benzothiazol-2-yl]-N-(2-sulfamoylethyl)acetamide	1591499: Inhibition of human endothelial lipase derived from human HT1080 cell conditioned media using PED-A1 as substrate incubated for 20 mins and measured every 20 secs for 10 mins by FRET assay	ic50	0.0100	uM
2-[(6-phenyl-1,3-benzothiazol-2-yl)-(3,3,3-trifluoropropylsulfonyl)methyl]-5-[(sulfamoylamino)methyl]-1,3,4-oxadiazole	1586813: Inhibition of endothelial lipase in human HT1080 cells using PED-A1 containing DMPG vesicles as substrate pretreated for 20 mins followed by substrate addition and measured every 20 secs for 10 mins by fluorescence assay	ic50	0.0100	uM
2-[benzylsulfonyl-[6-(3-chlorophenyl)-1,3-benzothiazol-2-yl]methyl]-5-[(sulfamoylamino)methyl]-1,3,4-oxadiazole	1586813: Inhibition of endothelial lipase in human HT1080 cells using PED-A1 containing DMPG vesicles as substrate pretreated for 20 mins followed by substrate addition and measured every 20 secs for 10 mins by fluorescence assay	ic50	0.0100	uM
2-[(6-phenyl-1,3-benzothiazol-2-yl)-propan-2-ylsulfonylmethyl]-5-[(sulfamoylamino)methyl]-1,3,4-oxadiazole	1586813: Inhibition of endothelial lipase in human HT1080 cells using PED-A1 containing DMPG vesicles as substrate pretreated for 20 mins followed by substrate addition and measured every 20 secs for 10 mins by fluorescence assay	ic50	0.0100	uM
2-[benzylsulfonyl-[6-(3,4-dichlorophenyl)-1,3-benzothiazol-2-yl]methyl]-5-[(sulfamoylamino)methyl]-1,3,4-oxadiazole	1586813: Inhibition of endothelial lipase in human HT1080 cells using PED-A1 containing DMPG vesicles as substrate pretreated for 20 mins followed by substrate addition and measured every 20 secs for 10 mins by fluorescence assay	ic50	0.0100	uM
4-[2-[benzylsulfonyl-[5-[(sulfamoylamino)methyl]-1,3,4-oxadiazol-2-yl]methyl]-1,3-benzothiazol-6-yl]-2-chloro-N,N-dimethylbenzamide	1586813: Inhibition of endothelial lipase in human HT1080 cells using PED-A1 containing DMPG vesicles as substrate pretreated for 20 mins followed by substrate addition and measured every 20 secs for 10 mins by fluorescence assay	ic50	0.0100	uM
5-[[5-[methylsulfonyl-(6-phenyl-1,3-benzothiazol-2-yl)methyl]-1,3,4-oxadiazol-2-yl]methyl]-1,3-thiazolidine-2,4-dione	1586813: Inhibition of endothelial lipase in human HT1080 cells using PED-A1 containing DMPG vesicles as substrate pretreated for 20 mins followed by substrate addition and measured every 20 secs for 10 mins by fluorescence assay	ic50	0.0100	uM
2-[2-methoxyethylsulfonyl-(6-phenyl-1,3-benzothiazol-2-yl)methyl]-5-[(sulfamoylamino)methyl]-1,3,4-oxadiazole	1586813: Inhibition of endothelial lipase in human HT1080 cells using PED-A1 containing DMPG vesicles as substrate pretreated for 20 mins followed by substrate addition and measured every 20 secs for 10 mins by fluorescence assay	ic50	0.0100	uM
4-[4-[2-[benzylsulfonyl-[5-[(sulfamoylamino)methyl]-1,3,4-oxadiazol-2-yl]methyl]-1,3-benzothiazol-6-yl]-2-chlorobenzoyl]morpholine	1586813: Inhibition of endothelial lipase in human HT1080 cells using PED-A1 containing DMPG vesicles as substrate pretreated for 20 mins followed by substrate addition and measured every 20 secs for 10 mins by fluorescence assay	ic50	0.0100	uM
5-methyl-5-[[5-[methylsulfonyl-[6-[4-(morpholine-4-carbonyl)phenyl]-1,3-benzothiazol-2-yl]methyl]-1,3,4-oxadiazol-2-yl]methyl]imidazolidine-2,4-dione	1586813: Inhibition of endothelial lipase in human HT1080 cells using PED-A1 containing DMPG vesicles as substrate pretreated for 20 mins followed by substrate addition and measured every 20 secs for 10 mins by fluorescence assay	ic50	0.0120	uM
2-cyano-N-[2-(cyclopropylamino)-2-oxoethyl]-2-(6-phenyl-1,3-benzothiazol-2-yl)acetamide	1601382: Inhibition of endothelial lipase (unknown origin)	ic50	0.0130	uM
6-methoxy-2-(2-phenylethyl)-3-(trifluoromethyl)-1-azatricyclo[6.3.1.04,12]dodeca-2,4,6,8(12)-tetraene	1056400: Inhibition of human endothelial lipase using PLAi as substrate measured for 30 mins by cell-based fluorescence assay	ic50	0.0140	uM
2-[6-[4-(azetidine-1-carbonyl)phenyl]-1,3-benzothiazol-2-yl]-2-cyano-N-[2-(cyclopropylamino)-2-oxoethyl]acetamide	1601382: Inhibition of endothelial lipase (unknown origin)	ic50	0.0150	uM
2-cyano-N-[2-(cyclopropylamino)-2-oxoethyl]-2-[6-[3-(piperidine-1-carbonyl)phenyl]-1,3-benzothiazol-2-yl]acetamide	1601382: Inhibition of endothelial lipase (unknown origin)	ic50	0.0160	uM
5-amino-2,4-dioxo-N-[(1R)-5-phenylmethoxy-2,3-dihydro-1H-inden-1-yl]-1H-pyrimidine-6-carboxamide	1530293: Inhibition of recombinant human endothelial lipase expressed in African green monkey COS7 cells using HDL as substrate pretreated for 10 mins followed by substrate addition and measured after 30 mins by LC/MS/MS analysis	ic50	0.0170	uM
N-[3-(3,4-dichlorophenyl)propyl]-1-ethyl-5-oxo-4-(2-propan-2-yloxyethylamino)-2H-pyrrole-3-carboxamide	1384994: Inhibition of endothelial lipase in human HT1080 cells using PED-A1 containing DMPG vesicles as substrate pretreated for 20 mins followed by substrate addition and measured every 20 secs for 10 mins by fluorescence assay	ic50	0.0190	uM
N-[3-(3,4-dichlorophenyl)propyl]-4-hydroxy-5-oxo-1-[3-(2-oxopyrrolidin-1-yl)propyl]-2H-pyrrole-3-carboxamide	1384994: Inhibition of endothelial lipase in human HT1080 cells using PED-A1 containing DMPG vesicles as substrate pretreated for 20 mins followed by substrate addition and measured every 20 secs for 10 mins by fluorescence assay	ic50	0.0190	uM
2-[[methyl(sulfamoyl)amino]methyl]-5-(6-phenyl-1,3-benzothiazole-2-carbonyl)-1,3,4-oxadiazole	1529147: Inhibition of EL in human HT1080 cells using A10070 as substrate preincubated for 20 min followed by DMPG vesicle doped substrate addition and measured at 20 secs interval for 10 mins by fluorescence assay	ic50	0.0200	uM
[5-[(methylsulfamoylamino)methyl]-1,3,4-oxadiazol-2-yl]-(6-phenyl-1,3-benzothiazol-2-yl)methanone	1529147: Inhibition of EL in human HT1080 cells using A10070 as substrate preincubated for 20 min followed by DMPG vesicle doped substrate addition and measured at 20 secs interval for 10 mins by fluorescence assay	ic50	0.0200	uM
2-[6-(3-oxo-1,2-dihydroisoindol-5-yl)-1,3-benzothiazole-2-carbonyl]-5-[(sulfamoylamino)methyl]-1,3,4-oxadiazole	1529147: Inhibition of EL in human HT1080 cells using A10070 as substrate preincubated for 20 min followed by DMPG vesicle doped substrate addition and measured at 20 secs interval for 10 mins by fluorescence assay	ic50	0.0200	uM
5-amino-2,4-dioxo-N-[4-(4-phenylmethoxyphenyl)cyclohexyl]-1H-pyrimidine-6-carboxamide	1530293: Inhibition of recombinant human endothelial lipase expressed in African green monkey COS7 cells using HDL as substrate pretreated for 10 mins followed by substrate addition and measured after 30 mins by LC/MS/MS analysis	ic50	0.0210	uM
methyl N-[4-[2-[benzylsulfonyl-[5-[(sulfamoylamino)methyl]-1,3,4-oxadiazol-2-yl]methyl]-1,3-benzothiazol-6-yl]phenyl]carbamate	1586813: Inhibition of endothelial lipase in human HT1080 cells using PED-A1 containing DMPG vesicles as substrate pretreated for 20 mins followed by substrate addition and measured every 20 secs for 10 mins by fluorescence assay	ic50	0.0210	uM
S-[(5-phenyl-1,3,4-oxadiazol-2-yl)methyl] N-[5-(3,5-difluorophenoxy)pentyl]carbamothioate	746240: Time dependent inhibition of human EL (19 to 500) expressed in HEK293 cells using PED-A1 as substrate by spectrophotometry	ic50	0.0230	uM
2-benzylsulfonyl-N-[2-(cyclopropylamino)-2-oxoethyl]-2-[6-(6-fluoro-3-pyridinyl)-1,3-benzothiazol-2-yl]acetamide	1591499: Inhibition of human endothelial lipase derived from human HT1080 cell conditioned media using PED-A1 as substrate incubated for 20 mins and measured every 20 secs for 10 mins by FRET assay	ic50	0.0250	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
sodium arsenite	affects cotreatment, increases abundance, decreases expression	3
Benzo(a)pyrene	decreases expression, decreases methylation	3
Estradiol	increases expression, decreases expression, affects cotreatment	3
Resveratrol	affects cotreatment, decreases expression	2
Acetaminophen	decreases expression	2
Nickel	increases expression	2
Silicon Dioxide	increases expression	2
Valproic Acid	decreases expression	2
Cyclosporine	affects expression, decreases expression	2
Aflatoxin B1	affects expression, decreases expression	2
sotorasib	affects cotreatment, decreases expression	1
methyleugenol	decreases expression	1
bisphenol A	decreases expression, increases expression	1
2-methyl-4-isothiazolin-3-one	increases expression	1
ethyl-p-hydroxybenzoate	increases expression	1
o,p’-DDT	decreases expression	1
perfluorooctanoic acid	increases expression	1
benzo(e)pyrene	increases methylation	1
periodate-oxidized adenosine	affects expression	1
resorcinol	increases expression	1
hydroquinone	increases expression	1
1-O-hexadecyl-2-arachidonyl-sn-glycero-3-phosphocholine	increases hydrolysis	1
perfluoro-n-nonanoic acid	decreases expression	1
4-nitro-3-(octanoyloxy)benzoic acid	increases hydrolysis	1
monomethylarsonous acid	decreases expression	1
T0901317	increases expression	1
4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide	affects cotreatment, decreases expression	1
belinostat	affects cotreatment, decreases expression	1
ICG 001	decreases expression	1
ormosil	increases expression, affects binding	1

ChEMBL screening assays

51 unique, capped per target: 51 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1015044	Binding	Inhibition of endothelial lipase by cell based assay	Design, synthesis, and biological evaluation of (2R,alphaS)-3,4-dihydro-2-[3-(1,1,2,2-tetrafluoroethoxy)phenyl]-5-[3-(trifluoromethoxy)-phenyl]-alpha-(trifluoromethyl)-1(2H)-quinolineethanol as potent and orally active cholesteryl ester transfer protein inhibitor. — *J Med Chem*

Clinical trials (associated diseases)

Via MONDO — disease-level, not drug-specific.

Predicted chemistry — Sugi Predict

The predicted patent-compound landscape for LIPG across ~30M SureChEMBL compounds — explore on Sugi Predict.