LIPC

Summary

LIPC (lipase C, hepatic type, HGNC:6619) is a protein-coding gene on chromosome 15q21.3, encoding Hepatic triacylglycerol lipase (P11150). Catalyzes the hydrolysis of triglycerides and phospholipids present in circulating plasma lipoproteins, including chylomicrons, intermediate density lipoproteins (IDL), low density lipoproteins (LDL) of large size and high density lipoproteins (HDL), releasing free fatty acids (….

Enables glycerophospholipid phospholipase A1 activity and triacylglycerol lipase activity. Involved in several processes, including cholesterol homeostasis; plasma lipoprotein particle remodeling; and triglyceride catabolic process. Located in obsolete extracellular space. Implicated in several diseases, including Alzheimer’s disease; coronary artery disease; familial combined hyperlipidemia; peripheral vascular disease; and type 2 diabetes mellitus. Biomarker of hyperinsulinism; obesity; and type 1 diabetes mellitus.

Source: NCBI Gene 3990 — automated summary from GO annotations (Alliance of Genome Resources).

At a glance

• Gene–disease (curated): hyperlipidemia due to hepatic triglyceride lipase deficiency (Strong, GenCC)
• GWAS associations: 336 (top 1% of genes corpus-wide)
• Clinical variants (ClinVar): 357 total — 3 pathogenic, 1 likely-pathogenic (top 9% of genes corpus-wide)
• GTEx eGene: eQTL in 29 tissues, sQTL in 3 (q < 0.05)
• Phenotypes (HPO): 13
• ChEMBL bioactivity: 1 clinical-phase molecule tested; no curated mechanism-of-action drug
• Constraint (gnomAD): pLI 0.00 (LoF-tolerant), LOEUF 1.10 (unconstrained)
• MANE Select transcript: NM_000236

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:6619
Approved symbol	LIPC
Name	lipase C, hepatic type
Location	15q21.3
Locus type	gene with protein product
Status	Approved
Aliases	HL, HTGL
Ensembl gene	ENSG00000166035
Ensembl biotype	protein_coding
OMIM	151670
Entrez	3990

Gene structure

Transcript identifiers

Ensembl transcripts: 38 — 30 protein_coding, 5 nonsense_mediated_decay, 3 retained_intron

MANE Select: ENST00000299022

Transcript support level (Ensembl TSL; 1 = fully mRNA-supported): TSL 1: 3, TSL 2: 2, TSL 3: 1, TSL 5: 1

ENST00000299022, ENST00000356113, ENST00000414170, ENST00000433326, ENST00000559845, ENST00000560257, ENST00000560664, ENST00000901639, ENST00000901640, ENST00000901641, ENST00000901642, ENST00000901643, ENST00000901644, ENST00000901645, ENST00000901646, ENST00000901647, ENST00000901648, ENST00000901649, ENST00000901650, ENST00000901651, ENST00000901652, ENST00000901653, ENST00000901654, ENST00000901655, ENST00000901656, ENST00000901657, ENST00000995557, ENST00000995562, ENST00000995564, ENST00000995565, ENST00000995566, ENST00001093729, ENST00001093730, ENST00001105994, ENST00001130348, ENST00001130349, ENST00001130350, ENST00001133132

RefSeq mRNA: 1 — MANE Select: NM_000236 NM_000236

CCDS: CCDS10166

Canonical transcript exons

ENST00000299022 — 9 exons

Exon	Start	End
ENSE00001099170	58563505	58563723
ENSE00001141787	58538333	58538517
ENSE00001930067	58568716	58569844
ENSE00003468798	58541785	58541967
ENSE00003471180	58542534	58542651
ENSE00003548373	58560864	58560981
ENSE00003549295	58545742	58545975
ENSE00003583777	58431991	58432120
ENSE00003606177	58548330	58548572

Expression profiles

Bgee: expression breadth ubiquitous, 158 present calls, max score 96.29.

FANTOM5 (CAGE): breadth broad, TPM avg 1.3025 / max 190.4220, expressed in 280 samples.

Highest expression (Bgee): lobe of liver, liver, colonic epithelium, tibial nerve, male germ line stem cell (sensu Vertebrata) in testis.

Genetic regulation across tissues (GTEx eQTL / sQTL)

LIPC is an eGene in GTEx v10 — its expression is genetically regulated (eQTL) in 29 tissues and its splicing (sQTL) in 3 (q < 0.05). Strongest associations first; slope = normalized effect of the lead variant’s alternative allele.

showing 20 of 32 significant tissue × QTL associations:

Tissue	QTL	q-value	Slope	Lead variant
Thyroid	eqtl	3.2e-46	+0.98	15:58410742:T:C
Whole Blood	eqtl	5.0e-41	+0.99	15:58478324:C:T
Esophagus Mucosa	eqtl	1.6e-26	+0.81	15:58410742:T:C
Cells Cultured fibroblasts	eqtl	1.4e-23	+0.40	15:58410742:T:C
Nerve Tibial	sqtl	6.0e-18	+0.50	15:58565179:A:G
Lung	eqtl	9.0e-17	+0.69	15:58410742:T:C
Adipose Visceral Omentum	eqtl	1.8e-16	+0.62	15:58410742:T:C
Liver	sqtl	5.1e-16	-0.87	15:58565179:A:G
Heart Atrial Appendage	eqtl	1.5e-13	+0.64	15:58410742:T:C
Pituitary	eqtl	1.6e-12	+0.71	15:58410742:T:C
Esophagus Muscularis	eqtl	1.9e-11	+0.48	15:58410742:T:C
Skin Sun Exposed Lower leg	eqtl	4.7e-11	+0.32	15:58410742:T:C
Esophagus Gastroesophageal Junction	eqtl	7.7e-11	+0.54	15:58410742:T:C
Liver	eqtl	3.9e-09	-0.36	15:58431280:T:C
Spleen	eqtl	4.5e-08	+0.76	15:58410742:T:C
Adipose Subcutaneous	eqtl	1.6e-07	+0.32	15:58410742:T:C
Pancreas	eqtl	2.1e-06	+0.44	15:58439368:A:G
Artery Aorta	eqtl	2.3e-06	+0.50	15:58410742:T:C
Colon Sigmoid	eqtl	3.4e-06	+0.49	15:58410742:T:C
Breast Mammary Tissue	eqtl	5.2e-06	+0.44	15:58410742:T:C

FANTOM5 promoters

4 alternative TSS:

Promoter ID	TPM avg	Samples expressed
146937	0.6502	232
146939	0.4430	41
146938	0.1984	42
207540	0.0109	4

Top tissues by expression

showing 100 of 286 tissues by Bgee expression score (0-100, higher = more expressed):

Tissue	Anatomy ID	Expression score	Quality
right lobe of liver	UBERON:0001114	96.29	gold quality
liver	UBERON:0002107	95.89	gold quality
colonic epithelium	UBERON:0000397	93.92	gold quality
tibial nerve	UBERON:0001323	77.77	gold quality
male germ line stem cell (sensu Vertebrata) in testis	CL:0000089 ∩ UBERON:0000473	76.95	silver quality
metanephros cortex	UBERON:0010533	75.33	gold quality
monocyte	CL:0000576	74.47	gold quality
mononuclear cell	CL:0000842	74.24	gold quality
sural nerve	UBERON:0015488	73.84	gold quality
leukocyte	CL:0000738	73.64	gold quality
adult mammalian kidney	UBERON:0000082	69.84	gold quality
kidney	UBERON:0002113	67.33	gold quality
cortex of kidney	UBERON:0001225	67.11	gold quality
islet of Langerhans	UBERON:0000006	65.94	gold quality
C1 segment of cervical spinal cord	UBERON:0006469	65.70	gold quality
mucosa of transverse colon	UBERON:0004991	65.58	gold quality
calcaneal tendon	UBERON:0003701	65.47	gold quality
metanephros	UBERON:0000081	64.41	gold quality
granulocyte	CL:0000094	64.10	gold quality
stromal cell of endometrium	CL:0002255	63.60	gold quality
spinal cord	UBERON:0002240	63.12	gold quality
renal glomerulus	UBERON:0000074	62.62	silver quality
right atrium auricular region	UBERON:0006631	62.62	gold quality
cardiac atrium	UBERON:0002081	61.53	gold quality
pancreas	UBERON:0001264	61.36	gold quality
gall bladder	UBERON:0002110	60.99	gold quality
prefrontal cortex	UBERON:0000451	60.84	gold quality
rectum	UBERON:0001052	60.83	gold quality
metanephric glomerulus	UBERON:0004736	60.80	gold quality
bone marrow cell	CL:0002092	60.78	silver quality
skin of hip	UBERON:0001554	59.42	silver quality
body of pancreas	UBERON:0001150	58.64	gold quality
apex of heart	UBERON:0002098	58.36	gold quality
blood	UBERON:0000178	57.97	gold quality
pituitary gland	UBERON:0000007	57.88	gold quality
upper leg skin	UBERON:0004262	57.17	silver quality
adult organism	UBERON:0007023	57.14	silver quality
heart left ventricle	UBERON:0002084	57.06	gold quality
mucosa of stomach	UBERON:0001199	56.97	gold quality
heart	UBERON:0000948	56.96	gold quality
lymph node	UBERON:0000029	56.68	gold quality
cardiac ventricle	UBERON:0002082	56.50	gold quality
tendon	UBERON:0000043	56.40	gold quality
adenohypophysis	UBERON:0002196	55.89	gold quality
transverse colon	UBERON:0001157	55.19	gold quality
tonsil	UBERON:0002372	54.72	gold quality
urinary bladder	UBERON:0001255	54.70	gold quality
frontal cortex	UBERON:0001870	54.38	gold quality
duodenum	UBERON:0002114	53.75	gold quality
Brodmann (1909) area 9	UBERON:0013540	53.67	gold quality
neocortex	UBERON:0001950	53.41	gold quality
right lung	UBERON:0002167	53.29	gold quality
small intestine	UBERON:0002108	53.13	gold quality
olfactory segment of nasal mucosa	UBERON:0005386	53.10	gold quality
spleen	UBERON:0002106	52.86	gold quality
cingulate cortex	UBERON:0003027	52.81	gold quality
adrenal tissue	UBERON:0018303	52.77	gold quality
uterine cervix	UBERON:0000002	52.65	gold quality
right coronary artery	UBERON:0001625	52.64	gold quality
substantia nigra	UBERON:0002038	52.61	gold quality
anterior cingulate cortex	UBERON:0009835	52.45	gold quality
thyroid gland	UBERON:0002046	52.29	gold quality
endocervix	UBERON:0000458	52.22	gold quality
left lobe of thyroid gland	UBERON:0001120	52.13	gold quality
stomach	UBERON:0000945	52.08	gold quality
right frontal lobe	UBERON:0002810	51.76	gold quality
lower esophagus mucosa	UBERON:0035834	51.60	gold quality
skin of leg	UBERON:0001511	51.58	gold quality
dorsolateral prefrontal cortex	UBERON:0009834	51.54	gold quality
small intestine Peyer’s patch	UBERON:0003454	51.43	gold quality
midbrain	UBERON:0001891	51.27	gold quality
fallopian tube	UBERON:0003889	51.21	gold quality
intestine	UBERON:0000160	51.20	gold quality
skin of abdomen	UBERON:0001416	51.04	gold quality
oocyte	CL:0000023	50.99	gold quality
cerebral cortex	UBERON:0000956	50.99	gold quality
amygdala	UBERON:0001876	50.92	gold quality
left coronary artery	UBERON:0001626	50.79	gold quality
zone of skin	UBERON:0000014	50.77	gold quality
colon	UBERON:0001155	50.69	gold quality
large intestine	UBERON:0000059	50.46	gold quality
frontal pole	UBERON:0002795	50.41	gold quality
anatomical system	UBERON:0000467	50.38	gold quality
coronary artery	UBERON:0001621	50.34	gold quality
material anatomical entity	UBERON:0000465	50.30	gold quality
multicellular organism	UBERON:0000468	50.30	gold quality
middle frontal gyrus	UBERON:0002702	50.30	gold quality
hindlimb stylopod muscle	UBERON:0004252	50.24	gold quality
paraflocculus	UBERON:0005351	50.18	gold quality
Brodmann (1909) area 10	UBERON:0013541	50.18	gold quality
smooth muscle tissue	UBERON:0001135	50.04	gold quality
body of stomach	UBERON:0001161	49.96	gold quality
vermiform appendix	UBERON:0001154	49.90	gold quality
quadriceps femoris	UBERON:0001377	49.90	gold quality
right lobe of thyroid gland	UBERON:0001119	49.62	gold quality
vastus lateralis	UBERON:0001379	49.45	gold quality
Brodmann (1909) area 46	UBERON:0006483	49.30	gold quality
blood vessel layer	UBERON:0004797	49.29	gold quality
subcutaneous adipose tissue	UBERON:0002190	49.26	gold quality
cerebellar vermis	UBERON:0004720	49.25	gold quality

Single-cell (SCXA)

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

Experiment	Marker?	Max mean expression
E-GEOD-130473	yes	608.81
E-ANND-3	no	4.31

HPA expression

RNA tissue specificity: Tissue enriched

showing 60 of 74 HPA tissues / cells by nTPM:

Tissue / cell	Axis	nTPM
Liver	tissue	159.9
Kidney	tissue	5.6
Spinal cord	tissue	3.3
Pancreas	tissue	2.3
Hippocampus	tissue	2.1
Superior colliculi	tissue	2.0
Thymus	tissue	2.0
Postcentral gyrus	tissue	2.0
Cerebral cortex	tissue	1.7
Duodenum	tissue	1.7
Locus coeruleus	tissue	1.7
Somatosensory cortex	tissue	1.7
Substantia nigra	tissue	1.6
Urinary bladder	tissue	1.5
Nucleus accumbens	tissue	1.5
Medulla oblongata	tissue	1.5
Pituitary gland	tissue	1.4
Breast	tissue	1.4
Pons	tissue	1.4
Corpus callosum	tissue	1.4
Retrosplenial and cingulate cortex	tissue	1.4
Insular cortex	tissue	1.4
Prefrontal cortex	tissue	1.3
Midbrain	tissue	1.3
Temporal cortex	tissue	1.3
Motor cortex	tissue	1.2
Thalamus	tissue	1.2
Thyroid gland	tissue	1.2
Hippocampal formation	tissue	1.2
Entorhinal cortex	tissue	1.2
Occipital cortex	tissue	1.2
Putamen	tissue	1.1
Periaqueductal gray	tissue	1.1
Retrosplenial cortex	tissue	1.1
Choroid plexus	tissue	1.0
Fallopian tube	tissue	1.0
Ovary	tissue	0.9
Basal ganglia	tissue	0.9
Olfactory bulb	tissue	0.9
Septum	tissue	0.9
Seminal vesicle	tissue	0.8
Epididymis	tissue	0.8
Small intestine	tissue	0.8
Ventral forebrain	tissue	0.8
Lymph node	tissue	0.7
Rectum	tissue	0.7
Frontal cortex	tissue	0.7
Amygdala	tissue	0.7
Spleen	tissue	0.7
Gallbladder	tissue	0.7
Skin 1	tissue	0.6
Colon	tissue	0.6
Hypothalamus	tissue	0.6
Esophagus	tissue	0.5
Cerebellum	tissue	0.5
Cervix	tissue	0.4
Stomach 1	tissue	0.4
Heart muscle	tissue	0.4
Placenta	tissue	0.4
Vagina	tissue	0.3

Brain sub-regions (HPA Brain Atlas): detected in 189; highest nTPM — Cerebellar white matter (3.6), Anterior cochlear nucleus, ventral (3.4), Dorsal spinal cord (3.3), Lateral funiculus (white matter) (3.3), Anterior funiculus (white matter) (3.1).

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): CEBPA, CNBP, ESR1, HNF1A, HNF4A, NR2F2, PITX2, SREBF1, SREBF2, USF1, USF2

Functional genomics

gnomAD constraint: pLI 1.24e-10, LOEUF 1.1, missense Z -0.405 — population loss-of-function intolerance (pLI ≥ 0.9 = LoF-intolerant; lower LOEUF = more constrained). gnomAD

Regional missense constraint (gnomAD RMC): no regional variation along ENST00000299022 — one region, missense o/e 1.08.

Literature-anchored findings (GeneRIF, showing 40)

• The -514C/T polymorphism of the HL gene was found to be associated with variations in hepatic lipase activity and serum HDL-C levels. (PMID:11947893)
• synthesized in peritoneal macrophages (PMID:11971936)
• The T allele of the hepatic lipase-514 C/T polymorphism is related to changes in plasma lipids. The superficially paradoxical predisposition to CHD in males is attributable to impairment of TG rich lipoprotein metabolism and reverse cholesterol transport. (PMID:12006918)
• REVIEW: role in coronary artery disease (PMID:12235167)
• LIPC promoter is associated with a lowered HL activity and that this variation may contribute to the increased plasma HDL-C concentration (PMID:12364543)
• Results suggest that a T right curved arrow C substitution at -2 of the HL promoter may be associated with th e variation of HDL-cholesterol concentration and therefore affect the risk of CAD in Chinese. (PMID:12417924)
• REVIEW: potential impact of genetic determinants of hepatic lipase activity in modulating both the development of coronary and carotid atherosclerosis will be discussed based on hepatic lipase proposed roles in lipoprotein metabolism (PMID:12642787)
• Hepatic lipase C514T polymorphism and its relationship with coronary artery disease in Koreans. (PMID:12689525)
• the determinants of cell surface binding exist within the carboxyl terminal 70 amino acids of hepatic lipase, of which the last five residues play an important role (PMID:12700335)
• HL enzyme activities in 28 healthy subjects with well-controlled Type 1 diabetes, and their relationship with Lp(A-I) and Lp(A-I,A-II) (PMID:12777470)
• A174T and T383M mutations in exon 8 of the HL gene resulted in HL deficiency among the three related compound heterozygotes and was associated with a marked TG enrichment of LDL and HDL particles (PMID:12777476)
• Hepatic lipase promoter SNPs are associated with increased HDL cholesterol and, paradoxically, an increased risk of IHD after adjustment for HDL cholesterol, and particularly in individuals with apolipoprotein E epsilon43 genotype. (PMID:12798568)
• The HL gene may play an important role in the regulation of HDL-C levels from childhood to adulthood, especially in white males. (PMID:12860265)
• The TT genotype of HL mutation may serve as a protective factor against vascular disease by increasing HDL cholesterol levels in hemodialysis patients with higher CETP levels. (PMID:14531818)
• -514C>T polymorphism associates with plasma lipids according to dietary intake and ethnic background (PMID:14608050)
• Hepatic lipase has a direct role in regulating total plasma LDL concentrations as well as in the production of smaller, denser LDL from larger, more buoyant precursors. (PMID:14615390)
• white American men had higher hepatic lipase activity than black American and Japanese American men, related to ethnic differences in central adiposity but not LIPC allele frequency (PMID:14657196)
• hepatic lipase clears plasma cholesterol in LDL receptor-deficient “apoB-48-only” and “apoB-100-only” mice (PMID:14679168)
• ApoA-II appears to increase Hepatic Lipase association with HDL and inhibits lipid hydrolysis (PMID:14967812)
• role of C-480T polymorphism and serum HDL-cholesterol on risk of acute myocardial infarction in men (PMID:14985399)
• the -250G/A polymorphism in the HL gene is associated with significant variations in high-density lipoprotein C levels and coronary artery disease risk in males. (PMID:15099346)
• G-250G genotype of LIPC gene is risk factor for type 2 diabetes. Genes regulating lipid and lipoprotein metabolism may be potential candidate genes for type 2 diabetes. (PMID:15126514)
• -514C–>T gene polymorphism correlates with elevated fasting insulin concentrations in a German population. (PMID:15156410)
• High levels of catalytically active human hepatic lipase (HL) reduce atherosclerosis, whereas high levels of a catalytically inactive HL do not affect atherosclerosis in mice genetically deficient in low-density lipoprotein receptor and mouse HL. (PMID:15205216)
• hepatic lipase binds to heparan sulfate proteoglycans and has a profound HDL-lowering effect (PMID:15292235)
• This meta-analysis demonstrates the importance of the -514C–>T single nucleotide polymorphism in determining hepatic lipase activity and plasma HDL concentration and helps quantify the role that hepatic lipase plays in the metabolism of HDL cholesterol. (PMID:15292318)
• an anti-atherogenic role of the ligand-binding function of Hepatic lipase in vivo. (PMID:15304509)
• apoE increases the rate of HL-mediated phospholipid and triacylglycerol hydrolysis in rHDL (PMID:15379569)
• the opposite regulation of HL expression by fatty acids and statins is mediated via SREBP, possibly through interaction with upstream stimulatory factors (PMID:15721010)
• Effect of long-term hormone replacement therapy (HRT) on the progression of atherosclerosis in a 5-yr follow-up observational study of 88 postmenopausal women with different hepatic lipase genotypes. (PMID:15755868)
• Results show an improvement in insulin sensitivity in men with the -514T allele of the hepatic lipase promoter polymorphism, when monounsaturated fatty acids and carbohydrates are consumed instead of saturated fat. (PMID:15821100)
• The LIPC -514C allele was associated with higher hepatic lipase activity in sedentary and physically active states. (PMID:15983229)
• Polymorphic genotypes might increase the risk of developing diabetic nephropathy by slowing clearance of triglyceride-rich remnant lipoproteins (PMID:15983323)
• The LIPC promoter -514 C-T polymorphism is associated with a significantly reduced development of neointima after surgery. (PMID:16005462)
• Resuslts suggest that HL gene might be one of the important susceptibility genes of type 2 diabetes and the high incidence of type 2 diabetes could be explained by high frequency of -514T allele in the Japanese population. (PMID:16077949)
• HL activity was positively related with body mass index (P < 0.02) and waist/hip ratio (P < 0.05, multiple r = 0.74), but not with plasma adiponectin. (PMID:16122151)
• hepatic lipase (LIPC)-514TT genotype and overweight status, when occurring together, were associated with a 3-fold increase in risk of preeclampsia among Peruvian women (PMID:16316842)
• The influence of hepatic lipase C-480T polymorphism on coronary flow reserve in young men is independent of the plasma cholesterol level. (PMID:16330034)
• The -514C–>T polymorphism modulates the lipid-lowering response to bezafibrate, with a better effect in homozygous hyperlipemic subjects. (PMID:16338252)
• Plasma adiponectin levels are associated with increased hepatic lipase activity in Japanese hyperlipidemic men. (PMID:16419358)

Cross-species orthologs

19 orthologs

Organism	Symbol	Gene ID
danio_rerio	lipca	ENSDARG00000053476
danio_rerio	lipcb	ENSDARG00000090486
mus_musculus	Lipc	ENSMUSG00000032207
rattus_norvegicus	Lipc	ENSRNOG00000060338
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): LIPG (ENSG00000101670), PLA1A (ENSG00000144837), LIPH (ENSG00000163898), LPL (ENSG00000175445), PNLIP (ENSG00000175535), PNLIPRP1 (ENSG00000187021), LIPI (ENSG00000188992), PNLIPRP3 (ENSG00000203837), PNLIPRP2 (ENSG00000266200)

Mouse-model phenotypes

Observed phenotypes of the mouse ortholog (MGI:96216) from MGI (Alliance of Genome Resources) — knockout/mutant phenotypes, ranked by annotation count. 10 distinct phenotype terms.

Mouse phenotype (MP)	Records
increased circulating cholesterol level	2
abnormal circulating cholesterol level	1
small ovary	1
increased circulating triglyceride level	1
increased circulating HDL cholesterol level	1
abnormal reproductive system physiology	1
decreased litter size	1
decreased circulating corticosterone level	1
decreased ovulation rate	1
abnormal circulating phospholipid level	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

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
ADAM10	protein-coding	102
LIPC-AS1	ncRNA	101928694
AQP9	protein-coding	366

Protein

Protein identifiers

Hepatic triacylglycerol lipase — P11150 (reviewed: P11150)

Alternative names: Lipase member C, Lysophospholipase, Phospholipase A1

All UniProt accessions (3): E7EUJ1, E7EUK6, P11150

UniProt curated annotations — full annotation on UniProt →

Function. Catalyzes the hydrolysis of triglycerides and phospholipids present in circulating plasma lipoproteins, including chylomicrons, intermediate density lipoproteins (IDL), low density lipoproteins (LDL) of large size and high density lipoproteins (HDL), releasing free fatty acids (FFA) and smaller lipoprotein particles. Also exhibits lysophospholipase activity. Can hydrolyze both neutral lipid and phospholipid substrates but shows a greater binding affinity for neutral lipid substrates than phospholipid substrates. In native LDL, preferentially hydrolyzes the phosphatidylcholine species containing polyunsaturated fatty acids at sn-2 position.

Subunit / interactions. Homodimer.

Subcellular location. Secreted.

Disease relevance. Hepatic lipase deficiency (HL deficiency) [MIM:614025] A disorder characterized by elevated levels of beta-migrating very low density lipoproteins, and abnormally triglyceride-rich low and high density lipoproteins. The disease is caused by variants affecting the gene represented in this entry.

Activity regulation. Phospholipase A1 and triacylglycerol lipase are inhibited by sphingomyelin.

Polymorphism. Genetic variations in LIPC define the high density lipoprotein cholesterol level quantitative trait locus 12 (HDLCQ12) [MIM:612797]. Genetic variations in LIPC are associated with susceptibility to type 2 diabetes mellitus (T2D) [MIM:125853].

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

RefSeq proteins (1): NP_000227* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000734	TAG_lipase	Family
IPR001024	PLAT/LH2_dom	Domain
IPR002333	Lipase_hep	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-acyl-sn-glycero-3-phosphocholine + H2O = sn-glycerol 3-phosphocholine + a fatty acid + H(+) (RHEA:15177)
• 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 = 2,3-di-(9Z)-octadecenoyl-sn-glycerol + (9Z)-octadecenoate + H(+) (RHEA:38391)
• 1,2-di-(9Z-octadecenoyl)-sn-glycerol + H2O = 2-(9Z-octadecenoyl)-glycerol + (9Z)-octadecenoate + H(+) (RHEA:38511)
• 1,2,3-tri-(9Z-octadecenoyl)-glycerol + H2O = di-(9Z)-octadecenoylglycerol + (9Z)-octadecenoate + H(+) (RHEA:38575)
• 1,3-di-(9Z-octadecenoyl)-glycerol + H2O = 3-(9Z-octadecenoyl)-sn-glycerol + (9Z)-octadecenoate + H(+) (RHEA:38651)
• 1,2-di-(9Z-octadecenoyl)-sn-glycero-3-phosphocholine + H2O = (9Z-octadecenoyl)-sn-glycero-3-phosphocholine + (9Z)-octadecenoate + H(+) (RHEA:38699)
• 1-hexadecanoyl-sn-glycero-3-phosphocholine + H2O = sn-glycerol 3-phosphocholine + hexadecanoate + H(+) (RHEA:40435)
• 1,2,3-tributanoylglycerol + H2O = dibutanoylglycerol + butanoate + H(+) (RHEA:40475)
• 1-(9Z-octadecenoyl)-sn-glycero-3-phospho-L-serine + H2O = sn-glycero-3-phospho-L-serine + (9Z)-octadecenoate + H(+) (RHEA:40499)
• 1,2-dihexadecanoyl-sn-glycero-3-phosphocholine + H2O = hexadecanoyl-sn-glycero-3-phosphocholine + hexadecanoate + H(+) (RHEA:41384)

UniProt features (23 total): sequence variant 9, glycosylation site 4, active site 3, mutagenesis site 2, signal peptide 1, chain 1, domain 1, sequence conflict 1, region of interest 1

Structure

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-P11150-F1	82.03	0.61

Human Protein Atlas

Protein class: Enzymes, ENZYME proteins, Hydrolases, Metabolic proteins, Predicted secreted proteins, Disease related genes, Potential drug targets, Human disease related genes, Congenital disorders of metabolism, Congenital disorders of lipid/glycolipid metabolism

Protein evidence: Evidence at protein level

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
168	nucleophile
194	charge relay system
279	charge relay system

Glycosylation sites (4)

Type	Positions
N-linked (glcnac…) asparagine	397, 42, 78, 362

Mutagenesis-validated functional residues (2)

Position	Phenotype
255–276	loss of triglyceride hydrolase and phospholipase activity.
255–275	increased triglyceride hydrolase and reduced phospholipase activity.

Function

Pathways and Gene Ontology

Reactome pathways

2 curated (TAS) of 6; 0 disease pathways. Curated-first; evidence = TAS (manually curated) vs IEA (electronic inference).

6 pathways:

ID	Pathway	Evidence
R-HSA-8963889	Assembly of active LPL and LIPC lipase complexes	curated
R-HSA-8964026	Chylomicron clearance	curated
R-HSA-174824	Plasma lipoprotein assembly, remodeling, and clearance	—
R-HSA-8964043	Plasma lipoprotein clearance	—
R-HSA-8963899	Plasma lipoprotein remodeling	—
R-HSA-382551	Transport of small molecules	—

MSigDB gene sets: 215 (showing top): MODULE_172, GOBP_ACYLGLYCEROL_HOMEOSTASIS, GOBP_PHOSPHOLIPID_METABOLIC_PROCESS, GOBP_PHOSPHATIDYLCHOLINE_METABOLIC_PROCESS, GOBP_STEROL_HOMEOSTASIS, GOBP_ORGANOPHOSPHATE_METABOLIC_PROCESS, HNF1_Q6, GOBP_MONOCARBOXYLIC_ACID_METABOLIC_PROCESS, GOBP_ORGANIC_ACID_BIOSYNTHETIC_PROCESS, GOBP_ORGANIC_HYDROXY_COMPOUND_TRANSPORT, GOBP_LIPID_HOMEOSTASIS, GOBP_GLYCEROLIPID_METABOLIC_PROCESS, GOBP_SMALL_MOLECULE_BIOSYNTHETIC_PROCESS, GOBP_PLASMA_LIPOPROTEIN_PARTICLE_CLEARANCE, RGTTAMWNATT_HNF1_01

GO Biological Process (13): fatty acid biosynthetic process (GO:0006633), triglyceride catabolic process (GO:0019433), very-low-density lipoprotein particle remodeling (GO:0034372), intermediate-density lipoprotein particle remodeling (GO:0034373), low-density lipoprotein particle remodeling (GO:0034374), high-density lipoprotein particle remodeling (GO:0034375), chylomicron remnant clearance (GO:0034382), phosphatidylcholine catabolic process (GO:0034638), cholesterol homeostasis (GO:0042632), reverse cholesterol transport (GO:0043691), triglyceride homeostasis (GO:0070328), lipid metabolic process (GO:0006629), lipid catabolic process (GO:0016042)

GO Molecular Function (13): lipoprotein lipase activity (GO:0004465), glycerophospholipase activity (GO:0004620), phosphatidylcholine lysophospholipase A1 activity (GO:0004622), triacylglycerol lipase activity (GO:0004806), heparin binding (GO:0008201), glycerophospholipid phospholipase A1 activity (GO:0008970), low-density lipoprotein particle binding (GO:0030169), apolipoprotein binding (GO:0034185), protein binding (GO:0005515), lipase activity (GO:0016298), hydrolase activity (GO:0016787), metal ion binding (GO:0046872), carboxylic ester hydrolase activity (GO:0052689)

GO Cellular Component (3): extracellular region (GO:0005576), endoplasmic reticulum lumen (GO:0005788), high-density lipoprotein particle (GO:0034364)

Reactome top-level categories

4 top-level categories:

Category	Pathways
Plasma lipoprotein assembly, remodeling, and clearance	2
Plasma lipoprotein remodeling	1
Plasma lipoprotein clearance	1
Transport of small molecules	1

GO top-level categories

34 GO namespaces:

Category	Terms
triglyceride-rich lipoprotein particle remodeling	2
plasma lipoprotein particle remodeling	2
hydrolase activity, acting on ester bonds	2
fatty acid metabolic process	1
lipid biosynthetic process	1
monocarboxylic acid biosynthetic process	1
triglyceride metabolic process	1
acylglycerol catabolic process	1
triglyceride-rich lipoprotein particle clearance	1
phosphatidylcholine metabolic process	1
glycerophospholipid catabolic process	1
sterol homeostasis	1
cholesterol transport	1
acylglycerol homeostasis	1
primary metabolic process	1
lipid metabolic process	1
catabolic process	1
triacylglycerol lipase activity	1
phospholipase activity	1
lysophospholipase A1 activity	1
lipase activity	1
carboxylic ester hydrolase activity	1
glycosaminoglycan binding	1
sulfur compound binding	1
A1-type glycerophospholipase activity	1
lipoprotein particle binding	1
protein binding	1
binding	1
catalytic activity	1
cation binding	1
cellular anatomical structure	1
endoplasmic reticulum	1
intracellular organelle lumen	1
plasma lipoprotein particle	1

Experimentally-supported GO annotations

GO terms backed by direct experimental evidence (ECO experimental codes) — 9 of 30 annotations. The rest are phylogenetic / computational / electronic (IEA).

9 experimentally-supported GO terms:

GO term	NS	Evidence
cholesterol homeostasis	BP	mutant phenotype
fatty acid biosynthetic process	BP	direct assay
high-density lipoprotein particle remodeling	BP	mutant phenotype
low-density lipoprotein particle remodeling	BP	mutant phenotype
triglyceride catabolic process	BP	direct assay
triglyceride homeostasis	BP	mutant phenotype
very-low-density lipoprotein particle remodeling	BP	direct assay
glycerophospholipid phospholipase A1 activity	MF	direct assay
triacylglycerol lipase activity	MF	direct assay

Protein interactions and networks

STRING

showing 15 of 1,341 interactions by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
LIPC	LMF1	Q96S06	901
LIPC	CETP	P11597	889
LIPC	APOB	P04114	815
LIPC	LIPF	P07098	797
LIPC	APOC2	P02655	796
LIPC	APOA1	P02647	772
LIPC	LCAT	P04180	763
LIPC	APOC3	P02656	755
LIPC	SCGB1D2	O95969	754
LIPC	APOA5	Q6Q788	750
LIPC	PLTP	P55058	728
LIPC	APOE	P02649	719
LIPC	ABCA1	O95477	719
LIPC	LDLR	P01130	716
LIPC	ARMS2	P0C7Q2	716

IntAct

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

2 partners by confidence:

Partner	Interaction type	MIscore	Records
ATP4A	association	0.530	2
ADHFE1	physical association	0.370	1

BioGRID (11 interactions; top human partners by supporting records): ATP4A (Affinity Capture-MS; 2 records), MTMR1 (Affinity Capture-MS; 2 records), ADHFE1 (Two-hybrid), APOB (Reconstituted Complex), LMF1 (Affinity Capture-Western), LRP1 (Reconstituted Complex), PTP4A3 (Proximity Label-MS), TTC7A (Affinity Capture-MS), ZNF517 (Affinity Capture-MS)

Disease & clinical

Genetic variants

Variant evidence for LIPC: 357 ClinVar records (4 pathogenic / likely pathogenic); 2 PharmGKB clinical annotations; 336 GWAS associations. Per-variant detail is on Sugi Variant.

ClinVar

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

Classification	Count (floor)
Pathogenic	3
Likely pathogenic	1
Uncertain significance	193
Likely benign	75
Benign	51

Top pathogenic / likely-pathogenic (4)

Showing all 4 pathogenic / likely-pathogenic ClinVar records, ranked by ClinVar review status (expert panel → multiple submitters → single submitter), then by number of submitting labs.

Variant ID	HGVS	Classification	Review	Submitters
1705275	NM_000236.3(LIPC):c.1052-1G>C	Pathogenic	no assertion criteria provided	2
29776	NM_000236.3(LIPC):c.583G>A (p.Ala195Thr)	Pathogenic	no assertion criteria provided	1
1174131	NM_000236.3(LIPC):c.1068= (p.Phe356=)	Pathogenic	no assertion criteria provided	1
1705274	NM_000236.3(LIPC):c.748T>C (p.Phe250Leu)	Likely pathogenic	no assertion criteria provided	1

Per-variant reference — Sugi Variant

Explore LIPC’s pathogenic and likely-pathogenic variants individually — each with its ClinVar classification and conditions, applied ACMG criteria (ClinGen expert panel, where curated), the calibrated in-silico predictors (AlphaMissense, REVEL, SaProt, conservation), gnomAD frequency, and the predictor-disagreement QC signal — on Sugi Variant.

SpliceAI

Top 10 splice-impact sites by Δscore (adjacent positions with the same effect merged into one range; 30 predictions of 997):

Position(s)	Effect	Δscore	Sites
15:58538465	donor_gain	1.0000
15:58541783–58541784	acceptor_loss	1.0000	5
15:58541968–58541969	donor_loss	1.0000	3
15:58548328–58548329	acceptor_loss	1.0000	6
15:58548573–58548574	donor_loss	1.0000	5
15:58556540	donor_gain	1.0000
15:58560862–58560863	acceptor_loss	1.0000	6
15:58563546	acceptor_gain	1.0000
15:58563549	acceptor_gain	1.0000
15:58563552	acceptor_gain	1.0000

AlphaMissense

732 missense substitutions predicted likely pathogenic (of 3,285 scored), across 198 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
D194	8	0.974	0.986
H279	8	0.949	0.983
S168	8	0.941	0.988
F200	8	0.931	0.990
H221	8	0.931	0.989
D242	8	0.913	0.962
D213	8	0.899	0.952
H172	8	0.879	0.956
D218	8	0.851	0.936
C254	7	0.978	0.992
C277	7	0.966	0.989
W122	7	0.956	0.987
C302	7	0.945	0.970
W90	7	0.924	0.978
F286	7	0.911	0.967
W99	7	0.909	0.974
C321	7	0.906	0.963
C313	7	0.904	0.958
N246	7	0.903	0.973
F349	7	0.890	0.972

HPA cancer prognostics

RNA cancer specificity: Group enriched (Kidney Renal Clear Cell Carcinoma, Kidney Renal Papillary Cell Carcinoma, Liver Hepatocellular Carcinoma)

Disease associations

OMIM: gene MIM:151670 | disease phenotypes: MIM:614025

GenCC curated gene-disease

1 curated gene-disease records:

Disease	Classification	Inheritance	Records
hyperlipidemia due to hepatic triglyceride lipase deficiency	Strong	Autosomal recessive	4

Genomics England panels (PanelApp)

Clinical diagnostic gene panels including this gene (6 panels, 0 green/diagnostic-grade). Confidence: green = diagnostic, amber = moderate.

6 panels:

Panel	Rating
Hypotonic infant	amber
Leukodystrophy, childhood onset	amber
Likely inborn error of metabolism	amber
Paediatric disorders	amber
Undiagnosed metabolic disorders	amber
Unexplained death in infancy and sudden unexplained death in childhood	amber

Mondo (1): hyperlipidemia due to hepatic triglyceride lipase deficiency (MONDO:0013533)

Orphanet (1): Hyperlipidemia due to hepatic triacylglycerol lipase deficiency (Orphanet:140905)

HPO phenotypes

13 phenotypes (HPO-id order):

HPO	Term
HP:0000006	Autosomal dominant inheritance
HP:0000007	Autosomal recessive inheritance
HP:0000855	Insulin resistance
HP:0001013	Eruptive xanthomas
HP:0001084	Corneal arcus
HP:0001681	Angina pectoris
HP:0002155	Hypertriglyceridemia
HP:0003124	Hypercholesterolemia
HP:0003584	Late onset
HP:0005181	Premature coronary artery atherosclerosis
HP:0005978	Type II diabetes mellitus
HP:0012184	Elevated circulating HDL-C concentration
HP:0031819	Increased waist to hip ratio

GWAS associations

showing 30 of 336 associations:

Study	Trait	p-value
GCST010241_207	Apolipoprotein A1 levels	0.000000e+00
GCST010242_118	HDL cholesterol levels	0.000000e+00
GCST010242_119	HDL cholesterol levels	0.000000e+00
GCST008075_65	HDL cholesterol levels x alcohol consumption (regular vs non-regular drinkers) interaction (2df)	3e-294
GCST008084_4	HDL cholesterol levels x alcohol consumption (drinkers vs non-drinkers) interaction (2df)	1e-218
GCST004232_45	HDL cholesterol levels	1e-213
GCST011348_64	High density lipoprotein cholesterol levels	3e-191
GCST002223_18	HDL cholesterol	1e-188
GCST010241_214	Apolipoprotein A1 levels	2e-186
GCST008075_206	HDL cholesterol levels x alcohol consumption (regular vs non-regular drinkers) interaction (2df)	4e-186
GCST010241_215	Apolipoprotein A1 levels	2e-173
GCST008085_165	HDL cholesterol levels in current drinkers	3e-163
GCST008084_160	HDL cholesterol levels x alcohol consumption (drinkers vs non-drinkers) interaction (2df)	6e-162
GCST006005_28	High density lipoprotein cholesterol levels	1e-140
GCST008070_53	HDL cholesterol levels	5e-124
GCST008084_103	HDL cholesterol levels x alcohol consumption (drinkers vs non-drinkers) interaction (2df)	7e-105
GCST001639_3	Metabolite levels	9e-104
GCST008075_3	HDL cholesterol levels x alcohol consumption (regular vs non-regular drinkers) interaction (2df)	3e-97
GCST009368_45	HDL cholesterol levels x long total sleep time interaction (2df test)	4e-97
GCST000755_28	HDL cholesterol	3e-96
GCST008085_30	HDL cholesterol levels in current drinkers	1e-94
GCST010242_65	HDL cholesterol levels	2e-93
GCST009368_20	HDL cholesterol levels x long total sleep time interaction (2df test)	6e-88
GCST009240_452	Serum metabolite levels (CMS)	1e-87
GCST003680_5	C-reactive protein levels or HDL-cholesterol levels (pleiotropy)	3e-87
GCST002899_38	HDL cholesterol	6e-87
GCST010244_2	Triglyceride levels	3e-86
GCST009240_451	Serum metabolite levels (CMS)	2e-85
GCST007827_4	Alzheimer’s disease or HDL levels (pleiotropy)	4e-84
GCST001392_15	Lipid metabolism phenotypes	7e-76

EFO canonical traits (from GWAS)

28 canonical traits:

EFO ID	Trait name
EFO:0004612	high density lipoprotein cholesterol measurement
EFO:0004530	triglyceride measurement
EFO:0004574	total cholesterol measurement
EFO:0004529	lipid measurement
EFO:0003926	neuropsychological test
EFO:0000195	metabolic syndrome
EFO:0004723	coronary artery calcification
EFO:0004338	body weight
EFO:0004509	hemoglobin measurement
EFO:0004725	metabolite measurement
EFO:1001492	atrophic macular degeneration
EFO:0004458	C-reactive protein measurement
EFO:0004611	low density lipoprotein cholesterol measurement
EFO:0009132	cholesterol efflux capacity measurement
EFO:0004329	alcohol drinking
EFO:0010225	lysophosphatidylethanolamine measurement
EFO:0010366	lysophosphatidylethanolamine 16:0 measurement
EFO:0007805	HDL cholesterol change measurement
EFO:0004614	apolipoprotein A 1 measurement
EFO:0004615	apolipoprotein B measurement
EFO:0007874	gut microbiome measurement
EFO:0004842	eosinophil count
EFO:0004348	hematocrit
EFO:0004587	lymphocyte count
EFO:0004305	erythrocyte count
EFO:0004736	aspartate aminotransferase measurement
EFO:0004533	alkaline phosphatase measurement
EFO:0004532	serum gamma-glutamyl transferase measurement

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL2127 (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)

PharmGKB clinical annotations

2 annotations by evidence level (1 strongest → 4):

Variant	Association	Level	Drugs	Phenotypes
rs1800588	Efficacy	3	fluvastatin;simvastatin
rs1800588	Efficacy	3	pravastatin

PharmGKB variants

1 variants:

Variant	Genes	Level	Score	#Clin annots	Drugs
rs1800588	LIPC	3	5.50	2	fluvastatin;simvastatin;pravastatin

PharmGKB variant annotations

Per-publication pharmacogenomic findings for this gene (significant associations).

3 published findings:

Variant	Drug(s)	Category	Finding	PMID
rs1800588	fluvastatin	Efficacy	Genotypes CC + CT are associated with increased response to fluvastatin as compared to genotype TT.	PMID:16103896
rs1800588	simvastatin	Efficacy	Genotype CT is associated with increased response to simvastatin as compared to genotype TT.	PMID:16103896
rs1800588	pravastatin	Efficacy	Genotypes CT + TT are associated with increased response to pravastatin in people with Hypercholesterolemia as compared to genotype CC.	PMID:16115483

Binding affinities (BindingDB)

287 measured of 409 human assays (410 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
CHEMBL4471611	IC50	1 nM
CHEMBL4460999	IC50	1 nM
2-[6-[1-(2-hydroxy-2-methylpropyl)-6-oxo-3-pyridinyl]-1,3-benzothiazol-2-yl]-2-methylsulfonyl-N-(2-sulfamoylethyl)acetamide	IC50	1.1 nM	US-8987314: Amide, urea or sulfone amide linked benzothiazole inhibitors of endothelial lipase
tert-butyl 4-[2-[1-benzylsulfonyl-2-oxo-2-(2-sulfamoylethylamino)ethyl]-1,3-benzothiazol-6-yl]benzoate	IC50	1.1 nM	US-8987314: Amide, urea or sulfone amide linked benzothiazole inhibitors of endothelial lipase
2-[5-(3-fluoro-4-pyridinyl)-1,3-benzothiazol-2-yl]-2-methylsulfonyl-N-(2-sulfamoylethyl)acetamide	IC50	1.1 nM	US-8987314: Amide, urea or sulfone amide linked benzothiazole inhibitors of endothelial lipase
2-methylsulfonyl-2-[6-(3-pyrrolidin-1-ylphenyl)-1,3-benzothiazol-2-yl]-N-(2-sulfamoylethyl)acetamide	IC50	1.2 nM	US-8987314: Amide, urea or sulfone amide linked benzothiazole inhibitors of endothelial lipase
4-[2-[1-[(3-cyanophenyl)methylsulfonyl]-2-oxo-2-(2-sulfamoylethylamino)ethyl]-1,3-benzothiazol-6-yl]-N-(2-methoxyethyl)benzamide	IC50	1.2 nM	US-8987314: Amide, urea or sulfone amide linked benzothiazole inhibitors of endothelial lipase
2-fluoro-N,N-dimethyl-4-[2-[1-methylsulfonyl-2-oxo-2-(2-sulfamoylethylamino)ethyl]-1,3-benzothiazol-6-yl]benzamide	IC50	1.2 nM	US-8987314: Amide, urea or sulfone amide linked benzothiazole inhibitors of endothelial lipase
2-[6-[4-(5-amino-1,3,4-thiadiazol-2-yl)phenyl]-1,3-benzothiazol-2-yl]-2-methylsulfonyl-N-(2-sulfamoylethyl)acetamide	IC50	1.2 nM	US-8987314: Amide, urea or sulfone amide linked benzothiazole inhibitors of endothelial lipase
4-[2-[1-benzylsulfonyl-2-oxo-2-(2-sulfamoylethylamino)ethyl]-5-methyl-1,3-benzothiazol-6-yl]benzoic acid	IC50	1.2 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]-2-(2-methoxyethylsulfonyl)-N-(2-sulfamoylethyl)acetamide	IC50	1.3 nM	US-8987314: Amide, urea or sulfone amide linked benzothiazole inhibitors of endothelial lipase
2-[6-(4-chlorophenyl)-1,3-benzothiazol-2-yl]-2-methylsulfonyl-N-(2-sulfamoylethyl)acetamide	IC50	1.4 nM	US-8987314: Amide, urea or sulfone amide linked benzothiazole inhibitors of endothelial lipase
tert-butyl 4-[2-[1-benzylsulfonyl-2-oxo-2-(2-sulfamoylethylamino)ethyl]-5-methyl-1,3-benzothiazol-6-yl]benzoate	IC50	1.4 nM	US-8987314: Amide, urea or sulfone amide linked benzothiazole inhibitors of endothelial lipase
BDBM151558	IC50	1.5 nM	US-8987314: Amide, urea or sulfone amide linked benzothiazole inhibitors of endothelial lipase
2-[6-[3-(4-hydroxypiperidine-1-carbonyl)phenyl]-1,3-benzothiazol-2-yl]-N-(2-sulfamoylethyl)-2-(3,3,3-trifluoropropylsulfonyl)acetamide	IC50	1.5 nM	US-8987314: Amide, urea or sulfone amide linked benzothiazole inhibitors of endothelial lipase
4-[2-[1-methylsulfonyl-2-oxo-2-(2-sulfamoylethylamino)ethyl]-1,3-benzothiazol-6-yl]benzamide	IC50	1.6 nM	US-8987314: Amide, urea or sulfone amide linked benzothiazole inhibitors of endothelial lipase
4-[5-methyl-2-[1-methylsulfonyl-2-oxo-2-(2-sulfamoylethylamino)ethyl]-1,3-benzothiazol-6-yl]benzoic acid	IC50	1.6 nM	US-8987314: Amide, urea or sulfone amide linked benzothiazole inhibitors of endothelial lipase
2-[6-(3,5-difluoro-4-methoxyphenyl)-1,3-benzothiazol-2-yl]-2-methylsulfonyl-N-(2-sulfamoylethyl)acetamide	IC50	1.7 nM	US-8987314: Amide, urea or sulfone amide linked benzothiazole inhibitors of endothelial lipase

ChEMBL bioactivities

376 potent at pChembl≥5 of 386 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
9.30	IC50	0.5	nM	CHEMBL3677564
9.10	IC50	0.8	nM	CHEMBL3677604
9.10	IC50	0.8	nM	CHEMBL3677538
9.10	IC50	0.8	nM	CHEMBL3677562
9.10	IC50	0.8	nM	CHEMBL4460999
9.00	IC50	1	nM	CHEMBL3677630
9.00	IC50	1	nM	CHEMBL3672652
8.85	IC50	1.4	nM	CHEMBL3677580
8.82	IC50	1.5	nM	CHEMBL3677632
8.72	IC50	1.9	nM	CHEMBL3672654
8.72	IC50	1.9	nM	CHEMBL3677540
8.70	IC50	2	nM	CHEMBL4463265
8.68	IC50	2.1	nM	CHEMBL3682478
8.66	IC50	2.2	nM	CHEMBL3677434
8.62	IC50	2.4	nM	CHEMBL3677571
8.59	IC50	2.6	nM	CHEMBL3677610
8.59	IC50	2.6	nM	CHEMBL3672653
8.59	IC50	2.6	nM	CHEMBL3677433
8.55	IC50	2.8	nM	CHEMBL3677607
8.55	IC50	2.8	nM	CHEMBL3677537
8.55	IC50	2.8	nM	CHEMBL3677550
8.54	IC50	2.9	nM	CHEMBL3677608
8.52	IC50	3	nM	CHEMBL3677543
8.52	IC50	3	nM	CHEMBL3677601
8.52	IC50	3	nM	CHEMBL3890635
8.52	IC50	3	nM	ORLISTAT
8.44	IC50	3.6	nM	CHEMBL3677563
8.44	IC50	3.6	nM	CHEMBL3677545
8.44	IC50	3.6	nM	CHEMBL3677547
8.40	IC50	4	nM	CHEMBL4465833
8.40	IC50	4	nM	CHEMBL4460376
8.30	IC50	5	nM	CHEMBL3905549
8.29	IC50	5.1	nM	CHEMBL3677602
8.28	IC50	5.2	nM	CHEMBL3677548
8.27	IC50	5.4	nM	CHEMBL4587475
8.17	IC50	6.7	nM	CHEMBL3682490
8.15	IC50	7.1	nM	CHEMBL3677439
8.15	IC50	7	nM	CHEMBL4437751
8.14	IC50	7.3	nM	CHEMBL3677567
8.11	IC50	7.7	nM	CHEMBL3677553
8.05	IC50	9	nM	CHEMBL4471611
8.03	IC50	9.4	nM	CHEMBL3677581
8.00	IC50	10	nM	CHEMBL3677462
8.00	IC50	10	nM	CHEMBL3672632
8.00	IC50	10	nM	CHEMBL3677554
8.00	IC50	10	nM	CHEMBL3982030
8.00	IC50	10	nM	CHEMBL4446812
8.00	IC50	10	nM	CHEMBL4440746
7.96	IC50	11	nM	CHEMBL3677480
7.96	IC50	11	nM	CHEMBL3677465

PubChem BioAssay actives

63 with measured affinity, of 90 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
benzyl N-[4-[2-[1-cyano-2-[[2-(cyclopropylamino)-2-oxoethyl]amino]-2-oxoethyl]-1,3-benzothiazol-6-yl]phenyl]carbamate	1601381: Inhibition of hepatic lipase (unknown origin)	ic50	0.0008	uM
2-(6-phenyl-1,3-benzothiazole-2-carbonyl)-5-[(sulfamoylamino)methyl]-1,3,4-oxadiazole	1529150: Inhibition of human HL expressed in human COS7 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	0.0020	uM
2-[[methyl(sulfamoyl)amino]methyl]-5-(6-phenyl-1,3-benzothiazole-2-carbonyl)-1,3,4-oxadiazole	1529150: Inhibition of human HL expressed in human COS7 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	0.0030	uM
Orlistat	1586814: Inhibition of recombinant human HL expressed in COS7 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	0.0030	uM
4-[6-fluoro-2-[5-[(sulfamoylamino)methyl]-1,3,4-oxadiazole-2-carbonyl]-1,3-benzothiazol-5-yl]-N-(2,2,2-trifluoroethyl)benzamide	1529150: Inhibition of human HL expressed in human COS7 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	0.0040	uM
5-fluoro-2-[5-[(sulfamoylamino)methyl]-1,3,4-oxadiazole-2-carbonyl]-N-(2,2,2-trifluoroethyl)-1,3-benzothiazole-6-carboxamide	1529150: Inhibition of human HL expressed in human COS7 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	0.0040	uM
methyl N-[4-[2-[5-[(sulfamoylamino)methyl]-1,3,4-oxadiazole-2-carbonyl]-1,3-benzothiazol-6-yl]phenyl]carbamate	1529150: Inhibition of human HL expressed in human COS7 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-phenyl-1,3-benzothiazol-2-yl)acetamide	1601381: Inhibition of hepatic lipase (unknown origin)	ic50	0.0054	uM
2-benzylsulfonyl-N-[2-(cyclopropylamino)-2-oxoethyl]-2-[6-(6-fluoro-3-pyridinyl)-1,3-benzothiazol-2-yl]acetamide	1591500: Inhibition of human hepatic lipase expressed in African green monkey COS7 cells using PED-A1 as substrate incubated for 20 mins and measured every 20 secs for 10 mins by FRET assay	ic50	0.0070	uM
2-[5-fluoro-6-(6-fluoro-3-pyridinyl)-1,3-benzothiazole-2-carbonyl]-5-[(sulfamoylamino)methyl]-1,3,4-oxadiazole	1529150: Inhibition of human HL expressed in human COS7 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	0.0090	uM
[5-[(methylsulfamoylamino)methyl]-1,3,4-oxadiazol-2-yl]-(6-phenyl-1,3-benzothiazol-2-yl)methanone	1529150: Inhibition of human HL expressed in human COS7 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
2-[6-(4-fluorophenyl)-1,3-benzothiazole-2-carbonyl]-5-[(sulfamoylamino)methyl]-1,3,4-oxadiazole	1529150: Inhibition of human HL expressed in human COS7 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
2-[(6-phenyl-1,3-benzothiazol-2-yl)-(3,3,3-trifluoropropylsulfonyl)methyl]-5-[(sulfamoylamino)methyl]-1,3,4-oxadiazole	1586814: Inhibition of recombinant human HL expressed in COS7 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	1586814: Inhibition of recombinant human HL expressed in COS7 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	1586814: Inhibition of recombinant human HL expressed in COS7 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	1586814: Inhibition of recombinant human HL expressed in COS7 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	1586814: Inhibition of recombinant human HL expressed in COS7 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	1586814: Inhibition of recombinant human HL expressed in COS7 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-phenyl-1,3-benzothiazol-2-yl)-N-(2-sulfamoylethyl)acetamide	1591500: Inhibition of human hepatic lipase expressed in African green monkey COS7 cells using PED-A1 as substrate incubated for 20 mins and measured every 20 secs for 10 mins by FRET assay	ic50	0.0150	uM
N-[3-(3,4-dichlorophenyl)propyl]-3-hydroxy-1-methyl-2-oxopyridine-4-carboxamide	1384995: Inhibition of recombinant human HL 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	0.0160	uM
2-[5-fluoro-6-(1-oxo-2,3-dihydroisoindol-5-yl)-1,3-benzothiazole-2-carbonyl]-5-[(sulfamoylamino)methyl]-1,3,4-oxadiazole	1529150: Inhibition of human HL expressed in human COS7 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-(6-fluoro-3-pyridinyl)-1,3-benzothiazole-2-carbonyl]-5-[(sulfamoylamino)methyl]-1,3,4-oxadiazole	1529150: Inhibition of human HL expressed in human COS7 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-fluoro-5-(1-oxo-2,3-dihydroisoindol-5-yl)-1,3-benzothiazole-2-carbonyl]-5-[(sulfamoylamino)methyl]-1,3,4-oxadiazole	1529150: Inhibition of human HL expressed in human COS7 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-[benzylsulfonyl-(6-phenyl-1,3-benzothiazol-2-yl)methyl]-5-[(sulfamoylamino)methyl]-1,3,4-oxadiazole	1586814: Inhibition of recombinant human HL expressed in COS7 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
2-(6-phenyl-1,3-benzothiazole-2-carbonyl)-5-[(1S)-1-(sulfamoylamino)ethyl]-1,3,4-oxadiazole	1529150: Inhibition of human HL expressed in human COS7 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	0.0300	uM
2-[6-(3-oxo-1,2-dihydroisoindol-5-yl)-1,3-benzothiazole-2-carbonyl]-5-[(sulfamoylamino)methyl]-1,3,4-oxadiazole	1529150: Inhibition of human HL expressed in human COS7 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	0.0300	uM
2-cyano-N-[2-(cyclopropylamino)-2-oxoethyl]-2-[6-[3-(piperidine-1-carbonyl)phenyl]-1,3-benzothiazol-2-yl]acetamide	1601381: Inhibition of hepatic lipase (unknown origin)	ic50	0.0350	uM
4-[2-fluoro-4-[5-fluoro-2-[5-[(sulfamoylamino)methyl]-1,3,4-oxadiazole-2-carbonyl]-1,3-benzothiazol-6-yl]benzoyl]morpholine	1529150: Inhibition of human HL expressed in human COS7 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	0.0400	uM
N-[2-(cyclopropylamino)-2-oxoethyl]-2-methylsulfonyl-2-(6-phenyl-1,3-benzothiazol-2-yl)acetamide	1591500: Inhibition of human hepatic lipase expressed in African green monkey COS7 cells using PED-A1 as substrate incubated for 20 mins and measured every 20 secs for 10 mins by FRET assay	ic50	0.0470	uM
2-methylsulfonyl-2-(6-phenyl-1,3-benzothiazol-2-yl)-N-(3-sulfamoylpropyl)acetamide	1591500: Inhibition of human hepatic lipase expressed in African green monkey COS7 cells using PED-A1 as substrate incubated for 20 mins and measured every 20 secs for 10 mins by FRET assay	ic50	0.0520	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	1586814: Inhibition of recombinant human HL expressed in COS7 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	0.0530	uM
2-[methylsulfonyl-(6-phenyl-1,3-benzothiazol-2-yl)methyl]-5-[(sulfamoylamino)methyl]-1,3,4-oxadiazole	1586814: Inhibition of recombinant human HL expressed in COS7 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	0.0530	uM
2-(6-phenyl-1,3-benzothiazole-2-carbonyl)-5-[(1R)-1-(sulfamoylamino)ethyl]-1,3,4-oxadiazole	1529150: Inhibition of human HL expressed in human COS7 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	0.0600	uM
2-cyano-N-[2-(cyclopropylamino)-2-oxoethyl]-2-[6-(1-oxo-2,3-dihydroisoindol-5-yl)-1,3-benzothiazol-2-yl]acetamide	1601381: Inhibition of hepatic lipase (unknown origin)	ic50	0.0700	uM
N-[3-(3,4-dichlorophenyl)propyl]-4-hydroxy-1-methyl-5-oxo-2H-pyrrole-3-carboxamide	1384995: Inhibition of recombinant human HL 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	0.0760	uM
N-[2-(cyclopropylamino)-2-oxoethyl]-2-[6-(6-fluoro-3-pyridinyl)-1,3-benzothiazol-2-yl]-2-(3,3,3-trifluoropropylsulfonyl)acetamide	1591500: Inhibition of human hepatic lipase expressed in African green monkey COS7 cells using PED-A1 as substrate incubated for 20 mins and measured every 20 secs for 10 mins by FRET assay	ic50	0.0790	uM
2-methylsulfonyl-2-(6-phenyl-1,3-benzothiazol-2-yl)-N-[2-(sulfamoylamino)ethyl]acetamide	1591500: Inhibition of human hepatic lipase expressed in African green monkey COS7 cells using PED-A1 as substrate incubated for 20 mins and measured every 20 secs for 10 mins by FRET assay	ic50	0.0810	uM
methyl N-[4-[2-[benzylsulfonyl-[5-[(sulfamoylamino)methyl]-1,3,4-oxadiazol-2-yl]methyl]-1,3-benzothiazol-6-yl]phenyl]carbamate	1586814: Inhibition of recombinant human HL expressed in COS7 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	0.0900	uM
4-[4-[2-[benzylsulfonyl-[5-[(sulfamoylamino)methyl]-1,3,4-oxadiazol-2-yl]methyl]-1,3-benzothiazol-6-yl]-2-chlorobenzoyl]morpholine	1586814: Inhibition of recombinant human HL expressed in COS7 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	0.1210	uM
N-[2-(cyclopropylamino)-2-oxoethyl]-2-[6-(6-fluoro-3-pyridinyl)-1,3-benzothiazol-2-yl]-2-methylsulfonylacetamide	1591500: Inhibition of human hepatic lipase expressed in African green monkey COS7 cells using PED-A1 as substrate incubated for 20 mins and measured every 20 secs for 10 mins by FRET assay	ic50	0.1300	uM
2-[6-[4-(azetidine-1-carbonyl)phenyl]-1,3-benzothiazol-2-yl]-2-cyano-N-[2-(cyclopropylamino)-2-oxoethyl]acetamide	1601381: Inhibition of hepatic lipase (unknown origin)	ic50	0.1700	uM
2-cyano-2-[6-(6-fluoro-3-pyridinyl)-1,3-benzothiazol-2-yl]-N-[2-(oxetan-3-ylamino)-2-oxoethyl]acetamide	1601381: Inhibition of hepatic lipase (unknown origin)	ic50	0.1900	uM
N-[2-(cyclopropylamino)-2-oxoethyl]-2-[6-(6-fluoro-3-pyridinyl)-1,3-benzothiazol-2-yl]-2-(2-methoxyethylsulfonyl)acetamide	1591500: Inhibition of human hepatic lipase expressed in African green monkey COS7 cells using PED-A1 as substrate incubated for 20 mins and measured every 20 secs for 10 mins by FRET assay	ic50	0.2300	uM
2-cyano-N-(2-oxo-2-pyrrolidin-1-ylethyl)-2-(6-phenyl-1,3-benzothiazol-2-yl)acetamide	1601381: Inhibition of hepatic lipase (unknown origin)	ic50	0.2500	uM
2-methylsulfonyl-2-[6-[4-(morpholine-4-carbonyl)phenyl]-1,3-benzothiazol-2-yl]-N-(2-sulfamoylethyl)acetamide	1591500: Inhibition of human hepatic lipase expressed in African green monkey COS7 cells using PED-A1 as substrate incubated for 20 mins and measured every 20 secs for 10 mins by FRET assay	ic50	0.2800	uM
2-cyano-N-[2-(cyclopropylamino)-2-oxoethyl]-2-[6-[4-(morpholine-4-carbonyl)phenyl]-1,3-benzothiazol-2-yl]acetamide	1601381: Inhibition of hepatic lipase (unknown origin)	ic50	0.3000	uM
2-methylsulfonyl-2-[6-[1-(2-morpholin-4-ylethyl)pyrazol-4-yl]-1,3-benzothiazol-2-yl]-N-(2-sulfamoylethyl)acetamide	1591500: Inhibition of human hepatic lipase expressed in African green monkey COS7 cells using PED-A1 as substrate incubated for 20 mins and measured every 20 secs for 10 mins by FRET assay	ic50	0.3100	uM
4-[2-[benzylsulfonyl-[5-[(sulfamoylamino)methyl]-1,3,4-oxadiazol-2-yl]methyl]-1,3-benzothiazol-6-yl]-2-chloro-N,N-dimethylbenzamide	1586814: Inhibition of recombinant human HL expressed in COS7 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	0.3910	uM
2-cyano-N-[2-(cyclopropylamino)-2-oxoethyl]-2-[6-(3-oxo-1,2-dihydroisoindol-5-yl)-1,3-benzothiazol-2-yl]acetamide	1601381: Inhibition of hepatic lipase (unknown origin)	ic50	0.4200	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	1586814: Inhibition of recombinant human HL expressed in COS7 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	0.4500	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
Benzo(a)pyrene	decreases expression, increases methylation	4
Cyclosporine	increases expression, affects cotreatment, decreases expression	4
bisphenol A	affects expression, increases expression, affects cotreatment	3
Tetrachlorodibenzodioxin	increases expression	3
Acetaminophen	decreases expression, affects cotreatment	2
Cholesterol, HDL	affects reaction, affects abundance	2
Valproic Acid	decreases expression, increases expression, increases methylation	2
Oleic Acid	increases expression, decreases expression, decreases reaction, affects cotreatment	2
aristolochic acid I	increases expression	1
GSK-J4	decreases expression	1
bisphenol F	affects cotreatment, increases expression	1
methyleugenol	decreases expression	1
pirinixic acid	affects binding, increases activity, increases expression	1
beta-lapachone	decreases expression	1
tris(1,3-dichloro-2-propyl)phosphate	decreases expression	1
butyraldehyde	decreases expression	1
perfluorooctanoic acid	decreases expression	1
ciglitazone	increases expression, affects binding	1
nefazodone	affects cotreatment, decreases expression	1
GW 4064	affects cotreatment, decreases expression	1
GW 501516	affects binding, increases expression	1
bazedoxifene	increases expression	1
obeticholic acid	decreases expression	1
6-(4-chlorophenyl)imidazo(2,1-b)(1,3)thiazole-5-carbaldehyde O-(3,4-dichlorobenzyl)oxime	affects cotreatment, increases expression	1
chiglitazar	increases expression	1
3-hydroxy-4-prenyl-5-methoxystilbene-2-carboxylic acid	increases expression	1
(+)-JQ1 compound	decreases expression	1
Atazanavir Sulfate	affects cotreatment, decreases expression	1
Rosiglitazone	increases expression	1
Sorafenib	decreases expression, decreases reaction	1

ChEMBL screening assays

12 unique, capped per target: 11 binding, 1 admet

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1015041	Binding	Inhibition of hepatic lipase activity assessed as release of free fatty acid from hydrolysis of VLDL 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*
CHEMBL4400383	ADMET	Inhibition of hepatic lipase (unknown origin)	Benzothiazole-based compounds as potent endothelial lipase inhibitors. — *Bioorg Med Chem Lett*

Clinical trials (associated diseases)

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

showing 60 of 300 trials:

NCT	Phase	Status	Title
NCT00006163	Phase 4	COMPLETED	Computer-assisted Diabetes Self-management Interventions
NCT00036504	Phase 4	COMPLETED	Efficacy and Safety of Twice-Daily Insulin Lispro Low Mixture Compared to a Once-Daily Long Acting Insulin Comparator in Patients Who Have Been Using One or More Oral Antihyperglycemic Agents Without Insulin
NCT00044460	Phase 4	COMPLETED	Efficacy and Safety In Poorly Controlled Type 2 Diabetics
NCT00095446	Phase 4	COMPLETED	NovoLog Observation Trial in Subjects With Type 1 and Type 2 Diabetes
NCT00101751	Phase 4	COMPLETED	INITIATE Plus (INITiation of Insulin to Reach A1c TargEt) Study
NCT00110370	Phase 4	COMPLETED	Comparing Pre-Mixed Insulin With Insulin Glargine Combined With Rapid-Acting Insulin in Patients With Type 2 Diabetes
NCT00110448	Phase 4	COMPLETED	Japanese Primary Prevention of Atherosclerosis With Aspirin for Diabetes (JPAD) Trial
NCT00118950	Phase 4	COMPLETED	Effect of Metformin Versus Repaglinide Treatment in Non-Obese Type 2 Diabetic Patients Uncontrolled by Diet
NCT00118963	Phase 4	COMPLETED	Effect of Repaglinide Versus Metformin Treatment in Non-Obese Patients With Type-2-Diabetes
NCT00121966	Phase 4	COMPLETED	South Danish Diabetes Study: Evaluation of the Antidiabetic Treatment of Type 2 Diabetes Mellitus
NCT00123604	Phase 4	COMPLETED	Vascular Effects of Carvedilol Versus Metoprolol in Hypertensive Patients With Type 2 Diabetes
NCT00123643	Phase 4	COMPLETED	Vascular Effects of Rosiglitazone Versus Glyburide in Type 2 Diabetic Patients
NCT00124397	Phase 4	COMPLETED	Atorvastatin and Endothelial Function in Type 2 Diabetes Mellitus (ATTEND-Study)
NCT00129233	Phase 4	COMPLETED	Comparison of Valsartan With Amlodipine in Hypertensive Patients With Glucose Intolerance
NCT00133718	Phase 4	COMPLETED	A 2 Year Trial of Patients With Type 2 Diabetes Focusing on Cardiovascular Diagnostics and Metabolic Control
NCT00135070	Phase 4	TERMINATED	Hospital In-Patient Insulin Study
NCT00141232	Phase 4	COMPLETED	Evaluating Atorvastatin With Omega-3 Fatty Acids in Cardiovascular Risk Reduction in Patients With Type 2 Diabetes
NCT00144144	Phase 4	UNKNOWN	A Study on Ca Blocker Versus AII Antagonists in Hypertension With Type 2 Diabetes
NCT00149331	Phase 4	COMPLETED	The Effects of Two Education Strategies About Insulin on Patient Preferences and Perceptions About Insulin Therapy
NCT00162357	Phase 4	COMPLETED	Post-PCI:Cardiac Imaging in Patients With Diabetes to Detect Coronary Artery Blockages Previously Opened by Angioplasty
NCT00174681	Phase 4	COMPLETED	Tulip Study: Testing the Usefulness of Lantus When Initiated Prematurely In Patients With Type 2 Diabetes
NCT00174824	Phase 4	COMPLETED	Comparison of Insulin Glargine and NPH Human Insulin in Progression of Diabetic Retinopathy in Type 2 Diabetic Patients
NCT00177398	Phase 4	COMPLETED	Effect of Glargine Insulin on Glucose Control in Hospitalized Patients Who Receive Tube Feedings
NCT00179400	Phase 4	COMPLETED	The Role of Acute Combined PPAR Alpha and Gamma Stimulation on Insulin Action in Humans
NCT00184561	Phase 4	COMPLETED	Effectiveness and Safety of Biphasic Insulin Aspart 70/30 in Subjects With Type 2 Diabetes
NCT00184626	Phase 4	COMPLETED	Comparison of Insulin Glargine Versus Biphasic Insulin Aspart 30/70 or Biphasic Insulin Aspart 30/70 in Combination With Metformin in Subjects With Type 2 Diabetes.
NCT00191178	Phase 4	COMPLETED	Effects of Insulin in Perceived Mood Symptoms in Patients With Type 2 Diabetes
NCT00191282	Phase 4	COMPLETED	Hyperglycemia and Cardiovascular Outcomes With Type 2 Diabetes
NCT00191464	Phase 4	COMPLETED	Long-Term Effects of Insulin Plus Metformin Regimens on the Overall and Postprandial Glycemic Control of Patients With Type 2 Diabetes
NCT00192803	Phase 4	UNKNOWN	Non-Insulin Dependent Diabetes Mellitus (NIDDM) and Angiotensin Converting Enzyme 2 (ACE2): Diabetic Patients Treated With Antihypertensive Drugs
NCT00202033	Phase 4	COMPLETED	Impact of Self-Monitoring Blood Glucose Frequency on Glycemic Control in Patients With Type 2 Diabetes
NCT00205660	Phase 4	COMPLETED	Changes in Adiposity, Metabolic Measures From Atypicals to Aripiprazole
NCT00212290	Phase 4	COMPLETED	Insulin Resistance and Central Nervous System (CNS) Function in Type 2 Diabetes
NCT00212303	Phase 4	COMPLETED	Exercise Training in Type 2 Diabetes and Hypertension
NCT00225342	Phase 4	WITHDRAWN	Study Protocol for Rosiglitazone Versus Gliclazide in Diabetics With Angina
NCT00238472	Phase 4	COMPLETED	A Pilot Study to Evaluate the Effects of Nateglinide vs. Glibenclamide on Renal Hemodynamics and Albumin Excretion
NCT00239538	Phase 4	COMPLETED	SMOOTH - Blood Pressure Control in Diabetic/Obese Patients
NCT00240253	Phase 4	COMPLETED	A Study Evaluating the Efficacy and Safety of Adding Symlin® to Lantus® (Insulin Glargine) in Subjects With Type 2 Diabetes
NCT00240422	Phase 4	COMPLETED	Trial to Compare the Effects of Either Telmisartan (40-80 mg PO Once Daily) or Ramipril (5-10 mg PO Once Daily) on Renal Endothelial Dysfunction in Hypertensive Patients With Type 2 Diabetes
NCT00241085	Phase 4	COMPLETED	Effect of Valsartan on Proteinuria in Patients With Hypertension and Diabetes Mellitus
NCT00241605	Phase 4	COMPLETED	AVANDAMET Versus Metformin For Type 2 Diabetes Mellitus
NCT00254085	Phase 4	UNKNOWN	Substitution of First Phase Insulin Response in Patient With Type 2 Diabetes.
NCT00258804	Phase 4	COMPLETED	Insulin Glargine During and After the Period of Fasting in Ramadan
NCT00262548	Phase 4	COMPLETED	C-Reactive Protein (CRP) in Obese Diabetic Women
NCT00264589	Phase 4	COMPLETED	Exercise Training and Cardiovascular Function in Obesity and in Type 2 Diabetes
NCT00264901	Phase 4	COMPLETED	Comparison of Self Adjustment Versus Standard of Care Treatment in Subjects With Type 2 Diabetes
NCT00265746	Phase 4	WITHDRAWN	Prevention of Diabetes Mellitus Development in Women Who Had Already Experienced A Gestational Diabetes
NCT00268645	Phase 4	COMPLETED	Insulin Glargine in Type 2 Diabetes
NCT00272077	Phase 4	COMPLETED	Insulin Glargine in Type 2 Diabetes Mellitus
NCT00272831	Phase 4	COMPLETED	The Use of Cilostazol in Patients With Diabetic Nephropathy
NCT00274274	Phase 4	COMPLETED	Efficacy and Safety of a Fixed or a Flexible Supplementary Insulin Therapy in Type 2 Diabetes
NCT00279201	Phase 4	COMPLETED	The DURABLE Trial: Evaluating the Durability of Starter Insulin Regimens in Patients With Type 2 Diabetes (IOOV)
NCT00282360	Phase 4	COMPLETED	Effect of Metabolic Therapy in Patients With Chronic Ischemic Heart Disease
NCT00282451	Phase 4	COMPLETED	Effect of Biphasic Insulin Compared to Biphasic Insulin Combined With Insulin Aspart, With or Without Metformin in Type 2 Diabetes
NCT00283049	Phase 4	TERMINATED	Insulin Glargine Injection Treatment in Place of Thiazolidinedione (TZD), Sulfonylurea, or Metformin in Triple Agent Therapy for Type 2 Diabetes Mellitus (T2DM) Adult Subjects With Unsatisfactory Control
NCT00283777	Phase 4	COMPLETED	Chromium and Insulin Action
NCT00290394	Phase 4	COMPLETED	Ambulatory Blood Pressure Reduction After Rosiglitazone Treatment In Normotensive Type 2 Diabetic Patients
NCT00296296	Phase 4	COMPLETED	Immunosuppression Impact on the Metabolic Control of Kidney Transplant With Pre-Existing Type 2 Diabetes (DM)
NCT00300911	Phase 4	COMPLETED	Effects of Rosiglitazone on Plasma BNP Levels and Left Ventricular Dysfunction
NCT00306176	Phase 4	COMPLETED	Rosiglitazone and Exercise in Patients With Type 2 Diabetes Mellitus

Predicted chemistry — Sugi Predict

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