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
• Clinical variants (ClinVar): 244 total
• Druggable target: yes — 1 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_006033

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: 9 — 7 protein_coding, 1 non_stop_decay, 1 TEC

ENST00000261292, ENST00000427224, ENST00000577628, ENST00000579750, ENST00000580036, ENST00000583083, ENST00000623277, ENST00000931130, ENST00000959465

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.

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

277 total, 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

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

Regulation

Is transcription factor: no

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

miRNA regulators (miRDB)

97 targeting LIPG, 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-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

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)

Protein

Protein identifiers

Endothelial lipase — Q9Y5X9 (reviewed: Q9Y5X9)

Alternative names: Endothelial cell-derived lipase, Phospholipase A1

All UniProt accessions (5): Q9Y5X9, A0A075B751, B4DTR8, 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), 5 shown:

• 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

Experimental structures (PDB)

0 structures.

Predicted structure (AlphaFold)

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

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): 169 (nucleophile); 193 (charge relay system); 274 (charge relay system)

Ligand- & substrate-binding residues (1): 325–337

Disulfide bonds (5): 64–77, 252–272, 297–316, 308–311, 463–483

Glycosylation sites (5): 469, 491, 80, 136, 393

Function

Pathways and Gene Ontology

Reactome pathways

4 pathways

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

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 (13): 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), regulation of lipoprotein metabolic process (GO:0050746), 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 (5): extracellular region (GO:0005576), obsolete extracellular space (GO:0005615), early endosome (GO:0005769), Golgi apparatus (GO:0005794), cell surface (GO:0009986)

Reactome top-level categories

Rollup of top-3 pathways:

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

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
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
lipoprotein metabolic process	1
regulation of protein metabolic process	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

Protein interactions and networks

STRING

1190 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
LIPG	POU2F3	Q9UKI9	842
LIPG	APOA1	P02647	832
LIPG	ANGPTL3	Q9Y5C1	777
LIPG	CETP	P11597	764
LIPG	LCAT	P04180	692
LIPG	PLTP	P55058	673
LIPG	ANGPTL8	Q6UXH0	637
LIPG	ABCA1	O95477	625
LIPG	APOB	P04114	623
LIPG	APOA5	Q6Q788	620
LIPG	GALNT2	Q10471	605
LIPG	LPAR3	Q9UBY5	590
LIPG	GPIHBP1	Q8IV16	586
LIPG	APOC3	P02656	583
LIPG	SCARB1	Q8WTV0	577

IntAct

7 interactions, top by confidence:

A	B	Type	Score
ETNPPL	ZC3HC1	psi-mi:“MI:0914”(association)	0.560
LIPG	NRP1	psi-mi:“MI:0914”(association)	0.530
NEK4	E2F8	psi-mi:“MI:0914”(association)	0.350
LIPG	TOR1B	psi-mi:“MI:0914”(association)	0.350
LIPG		psi-mi:“MI:0915”(physical association)	0.000
EXOSC5	LIPG	psi-mi:“MI:0915”(physical association)	0.000

BioGRID (82): Lipg (Affinity Capture-Western), DNAJC13 (Affinity Capture-MS), TMED4 (Affinity Capture-MS), TUBB1 (Affinity Capture-MS), TMED9 (Affinity Capture-MS), TMED5 (Affinity Capture-MS), TRMT1 (Affinity Capture-MS), PLS1 (Affinity Capture-MS), PTPRS (Affinity Capture-MS), NRP1 (Affinity Capture-MS), TMED10 (Affinity Capture-MS), TMED2 (Affinity Capture-MS), CANX (Affinity Capture-MS), ITIH2 (Affinity Capture-MS), SDC2 (Affinity Capture-MS)

ESM2 similar proteins: A1A4K5, A2BGL3, J3RZ81, O46559, O46647, P06858, P07867, P11150, P11151, P11152, P11153, P11602, P13612, P22413, P27656, P28825, P49060, P49923, P55031, P97535, Q06000, Q08761, Q13219, Q16819, Q29524, Q2TBF2, Q32PY2, Q3SZ79, Q53H76, Q5E9H0, Q5NDE3, Q5NDE4, Q5NDE5, Q5NDE8, Q5RBQ5, Q5XGE9, Q641F6, Q64230, Q64610, Q6DBU8

Diamond homologs: A0A0M3KKW3, A2VBC4, C0HLL3, O46559, P06857, P07867, P0CH47, P0CH86, P0CH87, P0DMB4, P0DMB5, P0DMB7, P0DMB8, P0DPT0, P0DSI2, P11150, P11602, P27656, P29183, P49369, P51528, P53357, P54315, P54316, P81139, Q02157, Q06478, Q3SZ79, Q3ZU95, Q5BKQ4, Q5XGE9, Q68KK0, Q6NYZ4, Q6Q249, Q6Q250, Q6Q251, Q6Q252, Q6XZB0, Q7M3V3, Q7M3V4

SIGNOR signaling

0 interactions.

Disease & clinical

Clinical variants and AI predictions

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

Top pathogenic / likely-pathogenic (0)

SpliceAI

1627 predictions. Top by Δscore:

Variant	Effect	Δscore
18:49565467:C:G	donor_gain	1.0000
18:49565496:ACGG:A	donor_loss	1.0000
18:49565497:CGG:C	donor_loss	1.0000
18:49565498:GGTGA:G	donor_loss	1.0000
18:49565499:G:T	donor_loss	1.0000
18:49565500:T:G	donor_loss	1.0000
18:49567436:CTGCA:C	acceptor_loss	1.0000
18:49567437:TGCA:T	acceptor_loss	1.0000
18:49567438:GCA:G	acceptor_loss	1.0000
18:49567439:CAGA:C	acceptor_loss	1.0000
18:49567440:A:AG	acceptor_gain	1.0000
18:49567441:G:A	acceptor_loss	1.0000
18:49567441:G:GA	acceptor_gain	1.0000
18:49567441:GATGA:G	acceptor_gain	1.0000
18:49567603:G:GT	donor_gain	1.0000
18:49567617:TGCAG:T	donor_loss	1.0000
18:49567619:CAG:C	donor_loss	1.0000
18:49567620:AGG:A	donor_loss	1.0000
18:49567621:GGT:G	donor_loss	1.0000
18:49567622:G:GA	donor_loss	1.0000
18:49567623:T:A	donor_loss	1.0000
18:49567639:G:GT	donor_gain	1.0000
18:49569432:TATAG:T	acceptor_loss	1.0000
18:49569434:TA:T	acceptor_loss	1.0000
18:49569435:A:AC	acceptor_loss	1.0000
18:49569435:A:AG	acceptor_gain	1.0000
18:49569436:G:GA	acceptor_loss	1.0000
18:49569436:G:GG	acceptor_gain	1.0000
18:49569436:GGA:G	acceptor_gain	1.0000
18:49569549:G:A	donor_loss	1.0000

AlphaMissense

3333 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
18:49575455:C:G	H220D	0.998
18:49575551:T:A	C252S	0.998
18:49575552:G:C	C252S	0.998
18:49581448:G:C	R276P	0.998
18:49581510:T:A	C297S	0.998
18:49581510:T:C	C297R	0.998
18:49581511:G:C	C297S	0.998
18:49581512:C:G	C297W	0.998
18:49569540:G:C	R188P	0.997
18:49575375:A:G	D193G	0.997
18:49575378:C:A	P194H	0.997
18:49575392:T:C	F199L	0.997
18:49575394:T:A	F199L	0.997
18:49575394:T:G	F199L	0.997
18:49581435:T:A	C272S	0.997
18:49581436:G:C	C272S	0.997
18:49581460:T:C	L280P	0.997
18:49565493:T:A	W92R	0.996
18:49565493:T:C	W92R	0.996
18:49565495:G:C	W92C	0.996
18:49565495:G:T	W92C	0.996
18:49569482:A:C	S169R	0.996
18:49569483:G:T	S169I	0.996
18:49569484:C:A	S169R	0.996
18:49569484:C:G	S169R	0.996
18:49575420:T:A	L208H	0.996
18:49575507:G:A	G237D	0.996
18:49575551:T:C	C252R	0.996
18:49581511:G:A	C297Y	0.996
18:49581511:G:T	C297F	0.996

dbSNP variants (sampled 300 via entrez): RS1000023797 (18:49588369 G>A), RS1000147016 (18:49563698 G>C), RS1000239096 (18:49562786 C>A), RS1000244213 (18:49568669 C>T), RS1000288514 (18:49575282 T>A), RS1000361698 (18:49575571 G>A), RS1000366022 (18:49597889 C>A), RS1000537952 (18:49562080 C>A), RS1000566837 (18:49567234 G>A), RS1000630515 (18:49564432 A>G), RS1000842811 (18:49574585 A>C,G), RS1001035163 (18:49587234 G>A), RS1001045976 (18:49592416 G>A), RS1001174069 (18:49575672 G>A,C), RS1001193138 (18:49597092 C>T)

Disease associations

OMIM: gene MIM:603684 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

116 associations (top):

Study	Trait	p-value
GCST000133_4	HDL cholesterol	2.000000e-07
GCST000135_1	HDL cholesterol	6.000000e-12
GCST000240_2	HDL cholesterol	5.000000e-10
GCST000285_6	Cholesterol, total	2.000000e-11
GCST000288_3	HDL cholesterol	2.000000e-11
GCST000290_2	HDL cholesterol	7.000000e-15
GCST000533_31	Lipid metabolism phenotypes	2.000000e-08
GCST000533_32	Lipid metabolism phenotypes	7.000000e-16
GCST000533_35	Lipid metabolism phenotypes	1.000000e-09
GCST000533_36	Lipid metabolism phenotypes	5.000000e-13
GCST000533_37	Lipid metabolism phenotypes	1.000000e-09
GCST000533_38	Lipid metabolism phenotypes	4.000000e-10
GCST000533_6	Lipid metabolism phenotypes	6.000000e-14
GCST000533_7	Lipid metabolism phenotypes	2.000000e-11
GCST000755_29	HDL cholesterol	3.000000e-49
GCST000760_32	Cholesterol, total	2.000000e-19
GCST000805_2	HDL cholesterol	2.000000e-12
GCST001392_12	Lipid metabolism phenotypes	7.000000e-11
GCST001762_97	Obesity-related traits	7.000000e-06
GCST002023_5	Testicular germ cell tumor	5.000000e-06
GCST002221_64	Cholesterol, total	4.000000e-18
GCST002223_13	HDL cholesterol	1.000000e-44
GCST002896_14	Cholesterol, total	1.000000e-12
GCST002899_1	HDL cholesterol	8.000000e-36
GCST003215_5	HDL cholesterol	2.000000e-09
GCST003680_18	C-reactive protein levels or HDL-cholesterol levels (pleiotropy)	1.000000e-15
GCST003801_3	Response to selective serotonin reuptake inhibitors in depression	9.000000e-07
GCST004029_30	Angiotensin-converting enzyme inhibitor intolerance	2.000000e-06
GCST004207_1	HDL cholesterol	3.000000e-09
GCST004231_5	Total cholesterol levels	3.000000e-13

EFO canonical traits (16, from GWAS)

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

1 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 38,186 (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
CHEMBL175247	ORLISTAT	4	38,186

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

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)

1052 measured of 1239 human assays (1239 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
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
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
2,2,2-trifluoroethyl N-{4-[2- ({[(cyclopropyl- carbamoyl)methyl] carbamoyl}(2- methoxyethane- sulfonyl)methyl)- 5-fluoro-1,3- benzothiazol-6- yl]phenyl} carbamate	IC50	1 nM	US-10173991: Sulfone amide linked benzothiazole inhibitors of endothelial lipase
cyclopropylmethyl N-{4-[2- [(cyclopropyl- carbamoyl)methyl] carbamoyl} (propane-2-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	decreases expression, affects cotreatment, increases abundance	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	affects binding, increases expression	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)

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