NAPEPLD

Summary

NAPEPLD (N-acyl phosphatidylethanolamine phospholipase D, HGNC:21683) is a protein-coding gene on chromosome 7q22.1, encoding N-acyl-phosphatidylethanolamine-hydrolyzing phospholipase D (Q6IQ20). D-type phospholipase that hydrolyzes N-acyl-phosphatidylethanolamines (NAPEs) to produce bioactive N-acylethanolamines/fatty acid ethanolamides (NAEs/FAEs) and phosphatidic acid.

NAPEPLD is a phospholipase D type enzyme that catalyzes the release of N-acylethanolamine (NAE) from N-acyl-phosphatidylethanolamine (NAPE) in the second step of the biosynthesis of N-acylethanolamine (Okamoto et al., 2004 [PubMed 14634025]).

Source: NCBI Gene 222236 — RefSeq curated summary.

At a glance

• Clinical variants (ClinVar): 78 total — 1 pathogenic
• GTEx eGene: eQTL in 39 tissues, sQTL in 5 (q < 0.05)
• ChEMBL bioactivity: 1 clinical-phase molecule tested; no curated mechanism-of-action drug
• Constraint (gnomAD): pLI 0.00 (LoF-tolerant), LOEUF 0.80 (unconstrained)
• MANE Select transcript: NM_001122838
• Notable: 78 clinical variants but no curated precision-oncology (CIViC) evidence yet

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:21683
Approved symbol	NAPEPLD
Name	N-acyl phosphatidylethanolamine phospholipase D
Location	7q22.1
Locus type	gene with protein product
Status	Approved
Aliases	FMP30, C7orf18, NAPE-PLD
Ensembl gene	ENSG00000161048
Ensembl biotype	protein_coding
OMIM	612334
Entrez	222236

Gene structure

Transcript identifiers

Ensembl transcripts: 27 — 23 protein_coding, 2 retained_intron, 2 nonsense_mediated_decay

MANE Select: ENST00000465647

Transcript support level (Ensembl TSL; 1 = fully mRNA-supported): TSL 1: 4, TSL 2: 2, TSL 4: 2, TSL 5: 2

ENST00000465647, ENST00000341533, ENST00000414118, ENST00000417955, ENST00000418294, ENST00000420631, ENST00000422589, ENST00000425379, ENST00000427257, ENST00000479761, ENST00000873865, ENST00000873866, ENST00000873867, ENST00000873868, ENST00000873869, ENST00000873870, ENST00000873871, ENST00000873872, ENST00000873873, ENST00000873874, ENST00000873875, ENST00000965816, ENST00000965817, ENST00000965818, ENST00000976742, ENST00001113453, ENST00001139176

RefSeq mRNA: 21 — MANE Select: NM_001122838 NM_001122838, NM_001386176, NM_001386177, NM_001386179, NM_001386182, NM_001386185, NM_001386189, NM_001386190, NM_001386191, NM_001386193, NM_001386194, NM_001386204, NM_001386205, NM_001386207, NM_001386208, NM_001386209, NM_001386210, NM_001386211, NM_001386212, NM_001386213, NM_198990

CCDS: CCDS5729

Canonical transcript exons

ENST00000465647 — 5 exons

Exon	Start	End
ENSE00001056131	103115060	103115174
ENSE00001132741	103119577	103120223
ENSE00001375894	103148811	103149099
ENSE00003496286	103128483	103128792
ENSE00004794339	103099776	103103554

Expression profiles

Bgee: expression breadth ubiquitous, 134 present calls, max score 95.38.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 3.3350 / max 172.2434, expressed in 1161 samples.

Highest expression (Bgee): corpus callosum, ventricular zone, superior frontal gyrus, duodenum, primary visual cortex.

Genetic regulation across tissues (GTEx eQTL / sQTL)

NAPEPLD is an eGene in GTEx v10 — its expression is genetically regulated (eQTL) in 39 tissues and its splicing (sQTL) in 5 (q < 0.05). Strongest associations first; slope = normalized effect of the lead variant’s alternative allele.

showing 20 of 44 significant tissue × QTL associations:

Tissue	QTL	q-value	Slope	Lead variant
Cells Cultured fibroblasts	eqtl	8.8e-39	+0.65	7:103142628:T:C
Adipose Subcutaneous	eqtl	3.5e-28	+0.57	7:103144994:C:T
Esophagus Muscularis	eqtl	5.7e-26	+0.60	7:103149048:A:G
Thyroid	eqtl	2.0e-21	+0.57	7:103155184:C:A
Skin Sun Exposed Lower leg	eqtl	5.0e-19	+0.37	7:103149048:A:G
Artery Tibial	eqtl	1.5e-17	+0.41	7:103149048:A:G
Skin Not Sun Exposed Suprapubic	eqtl	1.7e-15	+0.36	7:103142628:T:C
Esophagus Mucosa	eqtl	2.9e-14	+0.43	7:103241045:G:A
Testis	eqtl	5.5e-14	+0.89	7:103101697:C:T
Muscle Skeletal	eqtl	1.3e-13	+0.39	7:103149048:A:G
Colon Sigmoid	eqtl	6.1e-11	+0.44	7:103241045:G:A
Adipose Visceral Omentum	eqtl	6.8e-10	-0.37	7:103408276:C:G
Breast Mammary Tissue	eqtl	1.1e-09	+0.39	7:103149048:A:G
Esophagus Gastroesophageal Junction	eqtl	4.2e-09	+0.48	7:103149048:A:G
Pituitary	eqtl	9.0e-08	-0.61	7:103351841:G:C
Lung	eqtl	7.8e-07	+0.34	7:103159979:A:G
Heart Atrial Appendage	eqtl	6.1e-06	+0.33	7:103235009:C:G
Stomach	eqtl	6.6e-06	+0.32	7:103141999:A:C
Nerve Tibial	eqtl	1.4e-05	-0.28	7:103371062:G:A
Spleen	eqtl	1.4e-05	-0.37	7:103015625:C:T

FANTOM5 promoters

5 alternative TSS:

Promoter ID	TPM avg	Samples expressed
85368	2.5003	997
85369	0.4008	204
85365	0.2102	75
85366	0.1545	78
85367	0.0691	29

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
corpus callosum	UBERON:0002336	95.38	gold quality
ventricular zone	UBERON:0003053	95.36	gold quality
superior frontal gyrus	UBERON:0002661	91.93	gold quality
duodenum	UBERON:0002114	90.66	gold quality
primary visual cortex	UBERON:0002436	90.53	gold quality
Brodmann (1909) area 9	UBERON:0013540	90.32	gold quality
prefrontal cortex	UBERON:0000451	90.05	gold quality
dorsolateral prefrontal cortex	UBERON:0009834	89.31	gold quality
rectum	UBERON:0001052	89.10	gold quality
frontal cortex	UBERON:0001870	88.88	gold quality
cerebellar cortex	UBERON:0002129	88.65	gold quality
cerebellar hemisphere	UBERON:0002245	88.63	gold quality
mucosa of transverse colon	UBERON:0004991	88.59	gold quality
cerebellum	UBERON:0002037	88.51	gold quality
cerebral cortex	UBERON:0000956	88.28	gold quality
right hemisphere of cerebellum	UBERON:0014890	88.22	gold quality
ganglionic eminence	UBERON:0004023	87.29	gold quality
metanephros cortex	UBERON:0010533	87.25	gold quality
right frontal lobe	UBERON:0002810	86.81	gold quality
anterior cingulate cortex	UBERON:0009835	86.68	gold quality
C1 segment of cervical spinal cord	UBERON:0006469	86.46	gold quality
brain	UBERON:0000955	86.19	gold quality
colonic epithelium	UBERON:0000397	86.12	gold quality
Ammon’s horn	UBERON:0001954	86.05	gold quality
adrenal tissue	UBERON:0018303	85.87	gold quality
substantia nigra	UBERON:0002038	85.68	gold quality
amygdala	UBERON:0001876	85.61	gold quality
kidney	UBERON:0002113	85.57	gold quality
temporal lobe	UBERON:0001871	85.53	gold quality
endometrium	UBERON:0001295	85.51	gold quality
adult mammalian kidney	UBERON:0000082	85.43	gold quality
cortex of kidney	UBERON:0001225	85.35	gold quality
putamen	UBERON:0001874	85.18	gold quality
caudate nucleus	UBERON:0001873	85.02	gold quality
male germ line stem cell (sensu Vertebrata) in testis	CL:0000089 ∩ UBERON:0000473	84.92	gold quality
right uterine tube	UBERON:0001302	84.73	gold quality
transverse colon	UBERON:0001157	84.52	gold quality
ovary	UBERON:0000992	84.35	gold quality
left ovary	UBERON:0002119	83.99	gold quality
right ovary	UBERON:0002118	83.79	gold quality
descending thoracic aorta	UBERON:0002345	83.77	gold quality
nucleus accumbens	UBERON:0001882	83.64	gold quality
right testis	UBERON:0004534	83.48	gold quality
testis	UBERON:0000473	83.45	gold quality
left testis	UBERON:0004533	83.25	gold quality
hypothalamus	UBERON:0001898	82.91	gold quality
spleen	UBERON:0002106	82.85	gold quality
intestine	UBERON:0000160	82.46	gold quality
thyroid gland	UBERON:0002046	82.42	gold quality
gall bladder	UBERON:0002110	82.33	gold quality
small intestine	UBERON:0002108	82.31	gold quality
right lobe of liver	UBERON:0001114	82.27	gold quality
colon	UBERON:0001155	82.17	gold quality
left lobe of thyroid gland	UBERON:0001120	82.06	gold quality
right lobe of thyroid gland	UBERON:0001119	81.89	gold quality
right coronary artery	UBERON:0001625	81.84	gold quality
liver	UBERON:0002107	81.78	gold quality
small intestine Peyer’s patch	UBERON:0003454	81.66	gold quality
stomach	UBERON:0000945	81.64	gold quality
calcaneal tendon	UBERON:0003701	81.55	gold quality
thoracic aorta	UBERON:0001515	81.37	gold quality
tibial nerve	UBERON:0001323	81.25	gold quality
ascending aorta	UBERON:0001496	81.22	gold quality
islet of Langerhans	UBERON:0000006	80.94	gold quality
fallopian tube	UBERON:0003889	80.87	gold quality
body of stomach	UBERON:0001161	80.79	gold quality
primordial germ cell in gonad	CL:0000670 ∩ UBERON:0000991	80.71	gold quality
smooth muscle tissue	UBERON:0001135	80.64	gold quality
pancreas	UBERON:0001264	80.54	gold quality
adrenal gland	UBERON:0002369	80.49	gold quality
muscle tissue	UBERON:0002385	80.40	gold quality
right adrenal gland cortex	UBERON:0035827	80.37	gold quality
popliteal artery	UBERON:0002250	80.36	gold quality
right adrenal gland	UBERON:0001233	80.35	gold quality
tibial artery	UBERON:0007610	80.35	gold quality
body of pancreas	UBERON:0001150	80.33	gold quality
fundus of stomach	UBERON:0001160	80.18	gold quality
skeletal muscle tissue	UBERON:0001134	80.12	gold quality
multicellular organism	UBERON:0000468	79.89	gold quality
left adrenal gland	UBERON:0001234	79.87	gold quality
urinary bladder	UBERON:0001255	79.86	gold quality
left adrenal gland cortex	UBERON:0035825	79.65	gold quality
lymph node	UBERON:0000029	79.55	gold quality
left coronary artery	UBERON:0001626	79.54	gold quality
cortical plate	UBERON:0005343	79.43	gold quality
endocervix	UBERON:0000458	78.99	gold quality
vermiform appendix	UBERON:0001154	78.83	gold quality
muscle layer of sigmoid colon	UBERON:0035805	78.62	gold quality
hindlimb stylopod muscle	UBERON:0004252	78.33	gold quality
prostate gland	UBERON:0002367	78.31	gold quality
muscle of leg	UBERON:0001383	78.24	gold quality
body of uterus	UBERON:0009853	78.04	gold quality
gastrocnemius	UBERON:0001388	78.03	gold quality
esophagogastric junction muscularis propria	UBERON:0035841	77.84	gold quality
uterine cervix	UBERON:0000002	77.67	gold quality
myometrium	UBERON:0001296	77.61	gold quality
lower esophagus muscularis layer	UBERON:0035833	77.41	gold quality
lower esophagus	UBERON:0013473	77.40	gold quality
adenohypophysis	UBERON:0002196	77.28	gold quality
pituitary gland	UBERON:0000007	77.25	gold quality

Single-cell (SCXA)

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

Experiment	Marker?	Max mean expression
E-ANND-3	yes	3.07
E-GEOD-99795	no	175.32

HPA expression

RNA tissue specificity: Low tissue specificity

showing 60 of 80 HPA tissues / cells by nTPM:

Tissue / cell	Axis	nTPM	Protein (IHC)
Cerebral cortex	tissue	48.0	low
Somatosensory cortex	tissue	48.0
Motor cortex	tissue	42.5
Occipital cortex	tissue	41.7
Prefrontal cortex	tissue	36.7
Corpus callosum	tissue	36.3
Retrosplenial and cingulate cortex	tissue	35.5
Hippocampal formation	tissue	34.3
Entorhinal cortex	tissue	33.6
Retrosplenial cortex	tissue	33.5
Postcentral gyrus	tissue	32.1
Temporal cortex	tissue	32.0
Insular cortex	tissue	30.6
Putamen	tissue	29.0
Midbrain	tissue	25.8
Thalamus	tissue	25.4
Nucleus accumbens	tissue	25.3
Ventral forebrain	tissue	24.5
Medulla oblongata	tissue	24.0
Superior colliculi	tissue	22.8
Substantia nigra	tissue	22.2
Pons	tissue	21.6
Septum	tissue	21.6
Basal ganglia	tissue	21.3	not detected
Hippocampus	tissue	21.3	not detected
Amygdala	tissue	19.2
Spinal cord	tissue	19.1
Periaqueductal gray	tissue	18.9
Hypothalamus	tissue	18.4
Locus coeruleus	tissue	17.6
Kidney	tissue	13.9	high
Duodenum	tissue	13.6	medium
Olfactory bulb	tissue	12.2
Choroid plexus	tissue	10.9
Stomach 1	tissue	9.3	medium
Cerebellum	tissue	9.3	medium
Small intestine	tissue	9.1	medium
Frontal cortex	tissue	8.0
Thyroid gland	tissue	7.7	medium
Colon	tissue	7.2	high
Rectum	tissue	7.0	medium
Liver	tissue	7.0	low
Ovary	tissue	6.6	medium
Testis	tissue	6.3	medium
Spleen	tissue	6.1	low
Parathyroid gland	tissue	5.6	not detected
Gallbladder	tissue	5.5	medium
Fallopian tube	tissue	5.0	medium
Retina	tissue	4.5
Adrenal gland	tissue	4.4	medium
Prostate	tissue	4.2	low
Heart muscle	tissue	3.7	medium
Endometrium 1	tissue	3.4	low
Appendix	tissue	3.4	low
Cervix	tissue	3.3	not detected
Urinary bladder	tissue	3.3	medium
Pancreas	tissue	3.3	medium
Seminal vesicle	tissue	3.2	medium
Caudate putamen	tissue	3.2
Lymph node	tissue	3.1	medium

Brain sub-regions (HPA Brain Atlas): detected in 192; highest nTPM — Parieto-temporal junction (white matter) (44.6), Corpus callosum, genu (white matter) (41.4), Corpus callosum, splenium (white matter) (41.4), Angular gyrus (white matter) (41.0), Occipital cortex (white matter) (41.0).

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): IRF6, SP1

miRNA regulators (miRDB)

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

showing 30 of 182 miRNAs:

miRNA	Max score	Avg score	miRNA target_count
HSA-MIR-6867-5P	100.00	82.21	3464
HSA-MIR-450A-1-3P	100.00	69.33	1837
HSA-MIR-3924	100.00	72.09	2394
HSA-MIR-4481	100.00	66.42	1669
HSA-MIR-8485	100.00	77.57	4731
HSA-MIR-1277-5P	100.00	73.95	5056
HSA-MIR-548C-3P	99.99	74.01	7587
HSA-MIR-4282	99.99	75.36	6408
HSA-MIR-3662	99.99	73.82	5684
HSA-MIR-3185	99.99	68.12	1959
HSA-MIR-4789-3P	99.99	70.75	2484
HSA-MIR-186-5P	99.99	70.83	3707
HSA-MIR-5696	99.98	72.36	4487
HSA-MIR-19A-3P	99.98	75.33	2762
HSA-MIR-19B-3P	99.98	75.44	2754
HSA-MIR-3148	99.97	75.06	6478
HSA-MIR-3688-3P	99.97	72.02	2834
HSA-MIR-302E	99.96	70.74	2669
HSA-MIR-6778-3P	99.96	67.29	2693
HSA-MIR-570-3P	99.96	72.41	4910
HSA-MIR-551B-5P	99.96	71.28	3493
HSA-MIR-548AJ-3P	99.96	73.38	5345
HSA-MIR-548X-3P	99.96	73.38	5345
HSA-MIR-96-5P	99.95	72.80	2140
HSA-MIR-548J-3P	99.94	72.61	4881
HSA-MIR-218-5P	99.93	72.22	2103
HSA-MIR-3143	99.93	71.96	3104
HSA-MIR-335-3P	99.93	73.36	4958
HSA-MIR-548AE-3P	99.93	72.66	4867
HSA-MIR-548AH-3P	99.93	72.54	4872

Functional genomics

gnomAD constraint: pLI 0.000796, LOEUF 0.801, missense Z 1.43 — population loss-of-function intolerance (pLI ≥ 0.9 = LoF-intolerant; lower LOEUF = more constrained). gnomAD

Regional missense constraint (gnomAD RMC): no regional variation along ENST00000465647 — one region, missense o/e 0.86.

Literature-anchored findings (GeneRIF, showing 12)

• The human NAPE-PLD was activated by phosphatidylethanolamine and inhibited by the beta-lactamase substrate nitrocefin. (PMID:19715685)
• During the menstrual cycle, NAPE-PLD immunoreactivity was down-regulated in the secretory epithelial gland compared to the proliferative epithelial gland and unaffected in the stroma. (PMID:20369362)
• a common haplotype in NAPEPLD, an enzyme involved in endocannabinoid synthesis, was protective against obesity. (PMID:20885390)
• The results of this study suggested that NAPEPLD was alterated in multip;e sclerosis. (PMID:21251115)
• NAPE-PLD expression increase steadily after infancy, peaking in adulthood. (PMID:22827915)
• The differential expression of NAPE-PLD and FAAH suggests that Anandamide could play an important role in the pathophysiology of preeclampsia. (PMID:23122699)
• a major physiological role of NAPE-PLD (PMID:24018423)
• our results do not support a clear role of FAAH, CNR1 and NAPE-PLD in BD and lithium response. (PMID:24126189)
• NAPE-PLD forms homodimers partly separated by an internal channel and uniquely adapted to associate with phospholipids. (PMID:25684574)
• The AC genotype and C allele of NAPE-PLD rs12540583 locus are risk factors for schizophrenia. (PMID:29652995)
• Transcriptome analysis revealed that deletion of NAPE-PLD activates a transcriptional program for nutrient transportation, including lipids and lipoproteins, and inactivates cell-cycle or mitosis-related genes in Caco-2 cells. (PMID:30399323)
• NAPE-PLD is target of thiazide diuretics for hypertension. Its internal channel promotes transport of the cofactor PLP across cell membranes. (PMID:39999832)

Cross-species orthologs

5 orthologs

Organism	Symbol	Gene ID
danio_rerio	napepld	ENSDARG00000009252
mus_musculus	Napepld	ENSMUSG00000044968
rattus_norvegicus	Napepld	ENSRNOG00000011363
caenorhabditis_elegans		WBGENE00021370
caenorhabditis_elegans		WBGENE00021371

Mouse-model phenotypes

Observed phenotypes of the mouse ortholog (MGI:2140885) from MGI (Alliance of Genome Resources) — knockout/mutant phenotypes, ranked by annotation count. 2 distinct phenotype terms.

Mouse phenotype (MP)	Records
abnormal lipid homeostasis	1
abnormal brain morphology	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
Mycobacterium tuberculosis variant bovis AF2122/97	P64760	100.0%	Diamond
Mycobacterium tuberculosis CDC1551	P9WKP2	100.0%	Diamond
Mycobacterium tuberculosis H37Rv	P9WKP3	100.0%	Diamond
Pongo abelii	Q5RCU3	98.2%	Diamond
Bos taurus	Q58CN9	90.5%	Diamond
Klebsiella pneumoniae	Q48412	46.2%	Diamond
Purpureocillium lilacinum	A0A179HLJ8	37.3%	Diamond
Saccharomyces cerevisiae S288C	Q02883	34.6%	Diamond

Genomic neighbors (locus context)

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

Symbol	Type	Entrez
FBXL13	protein-coding	222235
NFE4	ncRNA	58160
ARMC10	protein-coding	83787
DNAJC2	protein-coding	27000
PMPCB	protein-coding	9512
LRRC17	protein-coding	10234
FAM185A	protein-coding	222234
PSMC2	protein-coding	5701

Protein

Protein identifiers

N-acyl-phosphatidylethanolamine-hydrolyzing phospholipase D — Q6IQ20 (reviewed: Q6IQ20)

All UniProt accessions (3): Q6IQ20, C9JGB1, H0Y4Y2

UniProt curated annotations — full annotation on UniProt →

Function. D-type phospholipase that hydrolyzes N-acyl-phosphatidylethanolamines (NAPEs) to produce bioactive N-acylethanolamines/fatty acid ethanolamides (NAEs/FAEs) and phosphatidic acid. Cleaves the terminal phosphodiester bond of diacyl- and alkenylacyl-NAPEs, primarily playing a role in the generation of long-chain saturated and monounsaturated NAEs in the brain. May control NAPE homeostasis in dopaminergic neuron membranes and regulate neuron survival, partly through RAC1 activation. As a regulator of lipid metabolism in the adipose tissue, mediates the crosstalk between adipocytes, gut microbiota and immune cells to control body temperature and weight. In particular, regulates energy homeostasis by promoting cold-induced brown or beige adipocyte differentiation program to generate heat from fatty acids and glucose. Has limited D-type phospholipase activity toward N-acyl lyso-NAPEs.

Subunit / interactions. Homodimer. Bile acids promote the assembly of inactive monomers into an active dimer and enable catalysis.

Subcellular location. Golgi apparatus membrane. Early endosome membrane. Nucleus envelope. Nucleus. Nucleoplasm.

Tissue specificity. Widely expressed. Highest expression in brain, kidney and testis (at protein level). Expressed in adipose tissue (at protein level).

Activity regulation. Activated by divalent cations. Activated by bile acids and their conjugates, except for lithocholic acid which is rather inhibitory. Binding of deoxycholic acid favors the selective release of anandamide and likely other unsatured long FAEs. Inhibited by phosphatidylethanolamines.

Cofactor. Binds 2 zinc divalent cations per subunit.

Similarity. Belongs to the NAPE-PLD family.

RefSeq proteins (21): NP_001116310, NP_001373105, NP_001373106, NP_001373108, NP_001373111, NP_001373114, NP_001373118, NP_001373119, NP_001373120, NP_001373122, NP_001373123, NP_001373133, NP_001373134, NP_001373136, NP_001373137, NP_001373138, NP_001373139, NP_001373140, NP_001373141, NP_001373142, NP_945341 (=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR001279	Metallo-B-lactamas	Domain
IPR024884	NAPE-PLD	Family
IPR036866	RibonucZ/Hydroxyglut_hydro	Homologous_superfamily

Pfam: PF12706

Enzyme classification (BRENDA)

• EC 3.1.4.54 — N-acetylphosphatidylethanolamine-hydrolysing phospholipase D (BRENDA: 4 organisms, 50 substrates, 156 inhibitors, 35 Km, 0 kcat entries)

Substrate kinetics (BRENDA)

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

Substrate	Km (mM)	Measurements
N-PALMITOYL-1,2-DIOLEOYL-PHOSPHATIDYLETHANOLAMIN	0.002–0.0647	15
N-PALMITOYLPHOSPHATIDYLETHANOLAMINE	0.0017–0.045	10
DIFLUORIDO[2-(HEXYLOXY)-3-(PHOSPHONOOXY)PROPYL 5	0.004	1
DIFLUORIDO[2-(HEXYLOXY)-3-(PHOSPHONOOXY)PROPYL 5	0.003	1
FLAME-NAPE	0.0092	1
N-ARACHIDONOYL-1,2-DIOLEOYLPHOSPHATIDYLETHANOLAM	0.0028	1
N-ARACHIDONOYL-1-OLEOYL-2-LYSOPHOSPHATIDYLETHANO	0.004	1
N-ARACHIDONOYLPHOSPHATIDYLETHANOLAMINE	0.04	1
N-OLEOYL-1,2-DIOLEOYLPHOSPHATIDYLETHANOLAMINE	0.0029	1
N-PALMITOYL-1-PALMITOYL-2-LINOLEOYLPHOSPHATIDYLE	0.0033	1
N-PALMITOYL-1-PALMITOYL-2-LYSOPHOSPHATIDYLETHANO	0.004	1
N-STEAROYL-1,2-DIOLEOYLPHOSPHATIDYLETHANOLAMINE	0.0034	1

Catalyzed reactions (Rhea)

• an N-acyl-1,2-diacyl-sn-glycero-3-phosphoethanolamine + H2O = an N-acylethanolamine + a 1,2-diacyl-sn-glycero-3-phosphate + H(+) (RHEA:33159)
• N-(5Z,8Z,11Z,14Z-eicosatetraenoyl)-1,2-di-(9Z-octadecenoyl)-sn-glycero-3-phosphoethanolamine + H2O = N-(5Z,8Z,11Z,14Z-eicosatetraenoyl)-ethanolamine + 1,2-di-(9Z-octadecenoyl)-sn-glycero-3-phosphate + H(+) (RHEA:45528)
• N,1,2-tri-(9Z-octadecenoyl)-sn-glycero-3-phosphoethanolamine + H2O = N-(9Z-octadecenoyl) ethanolamine + 1,2-di-(9Z-octadecenoyl)-sn-glycero-3-phosphate + H(+) (RHEA:45532)
• N-octadecanoyl-1,2-di-(9Z-octadecenoyl)-sn-glycero-3-phosphoethanolamine + H2O = N-octadecanoyl ethanolamine + 1,2-di-(9Z-octadecenoyl)-sn-glycero-3-phosphate + H(+) (RHEA:45536)
• N-hexadecanoyl-1,2-di-(9Z-octadecenoyl)-sn-glycero-3-phosphoethanolamine + H2O = N-hexadecanoylethanolamine + 1,2-di-(9Z-octadecenoyl)-sn-glycero-3-phosphate + H(+) (RHEA:45540)
• N-(5Z,8Z,11Z,14Z-eicosatetraenoyl)-1-(9Z-octadecenoyl)-sn-glycero-3-phosphoethanolamine + H2O = N-(5Z,8Z,11Z,14Z-eicosatetraenoyl)-ethanolamine + 1-(9Z-octadecenoyl)-sn-glycero-3-phosphate + H(+) (RHEA:45544)
• N-tetradecanoyl-1,2-di-(9Z-octadecenoyl)-sn-glycero-3-phosphoethanolamine + H2O = N-tetradecanoylethanolamine + 1,2-di-(9Z-octadecenoyl)-sn-glycero-3-phosphate + H(+) (RHEA:45552)
• N-dodecanoyl-1,2-di-(9Z-octadecenoyl)-sn-glycero-3-phosphoethanolamine + H2O = N-dodecanoylethanolamine + 1,2-di-(9Z-octadecenoyl)-sn-glycero-3-phosphate + H(+) (RHEA:45556)
• N,1-dihexadecanoyl-sn-glycero-3-phosphoethanolamine + H2O = N-hexadecanoylethanolamine + 1-hexadecanoyl-sn-glycero-3-phosphate + H(+) (RHEA:45592)
• N,1-dihexadecanoyl-2-(9Z,12Z-octadecadienoyl)-sn-glycero-3-phosphoethanolamine + H2O = 1-hexadecanoyl-2-(9Z,12Z-octadecadienoyl)-sn-glycero-3-phosphate + N-hexadecanoylethanolamine + H(+) (RHEA:45596)
• N-decanoyl-1-hexadecanoyl-2-(9Z,12Z-octadecadienoyl)-sn-glycero-3-phosphoethanolamine + H2O = N-decanoyl ethanolamine + 1-hexadecanoyl-2-(9Z,12Z-octadecadienoyl)-sn-glycero-3-phosphate + H(+) (RHEA:45608)
• N-octanoyl-1-hexadecanoyl-2-(9Z,12Z-octadecadienoyl)-sn-glycero-3-phosphoethanolamine + H2O = N-octanoyl ethanolamine + 1-hexadecanoyl-2-(9Z,12Z-octadecadienoyl)-sn-glycero-3-phosphate + H(+) (RHEA:45612)

UniProt features (59 total): strand 20, binding site 13, helix 9, mutagenesis site 5, turn 4, sequence variant 2, sequence conflict 2, chain 1, region of interest 1, modified residue 1, compositionally biased region 1

Structure

Experimental structures (PDB)

4 structures by resolution:

PDB	Title	Method	Resolution (Å)
4QN9	Structure of human NAPE-PLD	X-RAY DIFFRACTION	2.65
8P90	TARGET COMPLEX 2	X-RAY DIFFRACTION	2.8
8PC4	MEMBRANE TARGET COMPLEX 1	X-RAY DIFFRACTION	2.85
8P96	TARGET COMPLEX 3	X-RAY DIFFRACTION	2.86

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q6IQ20-F1	87.36	0.78

Human Protein Atlas

Protein class: Enzymes, ENZYME proteins, Hydrolases, Predicted intracellular proteins

Protein evidence: Evidence at protein level

Subcellular location (HPA, imaging): cytosol

Antibody reliability (HPA): IH approved · IF uncertain

Functional residue map

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

Ligand- & substrate-binding residues (13)

Position	Role
260	deoxycholate
284	Zn(2+)
321	an N-acyl-1,2-diacyl-sn-glycero-3-phosphoethanolamine
343	Zn(2+)
348	deoxycholate
185	Zn(2+)
187	Zn(2+)
188	an N-acyl-1,2-diacyl-sn-glycero-3-phosphoethanolamine
189	Zn(2+)
190	Zn(2+)
253	Zn(2+)
256	deoxycholate

Post-translational modifications (1)

Type	Positions
N-acetylmethionine	1

Mutagenesis-validated functional residues (5)

Position	Phenotype
158	impairs homodimerization resulting in loss of activity; when associated with s-159.
159	impairs homodimerization resulting in loss of activity; when associated with s-158.
207	loss of activity.
257	impairs binding to bile acids resulting in loss of activity.
380	loss of activity.

Function

Pathways and Gene Ontology

Reactome pathways

1 curated (TAS) of 5; 5 disease pathways. Curated-first; evidence = TAS (manually curated) vs IEA (electronic inference).

5 pathways:

ID	Pathway	Evidence
R-HSA-2466712	Biosynthesis of A2E, implicated in retinal degradation ⚕	curated
R-HSA-1643685	Disease ⚕	—
R-HSA-2474795	Diseases associated with visual transduction ⚕	—
R-HSA-9675143	Diseases of the neuronal system ⚕	—
R-HSA-2453864	Retinoid cycle disease events ⚕	—

MSigDB gene sets: 228 (showing top): SHEPARD_BMYB_MORPHOLINO_UP, GOBP_RESPONSE_TO_ETHANOL, GOBP_PHOSPHOLIPID_METABOLIC_PROCESS, GOBP_REGULATION_OF_FAT_CELL_DIFFERENTIATION, GOBP_BEHAVIOR, GOBP_INFLAMMATORY_RESPONSE, GCANCTGNY_MYOD_Q6, GOBP_POSITIVE_REGULATION_OF_FAT_CELL_DIFFERENTIATION, GOBP_MODULATION_OF_PROCESS_OF_ANOTHER_ORGANISM, GOBP_ORGANOPHOSPHATE_METABOLIC_PROCESS, GOBP_REGULATION_OF_BROWN_FAT_CELL_DIFFERENTIATION, CAGCTG_AP4_Q5, YY1_Q6, GOBP_GLYCEROLIPID_METABOLIC_PROCESS, GOBP_POSITIVE_REGULATION_OF_RESPONSE_TO_EXTERNAL_STIMULUS

GO Biological Process (13): temperature homeostasis (GO:0001659), phospholipid catabolic process (GO:0009395), response to isolation stress (GO:0035900), response to ethanol (GO:0045471), host-mediated modulation of intestinal microbiota composition (GO:0048874), positive regulation of inflammatory response (GO:0050729), N-acylethanolamine metabolic process (GO:0070291), N-acylphosphatidylethanolamine metabolic process (GO:0070292), positive regulation of brown fat cell differentiation (GO:0090336), negative regulation of eating behavior (GO:1903999), lipid metabolic process (GO:0006629), phospholipid metabolic process (GO:0006644), lipid catabolic process (GO:0016042)

GO Molecular Function (7): zinc ion binding (GO:0008270), bile acid binding (GO:0032052), identical protein binding (GO:0042802), N-acylphosphatidylethanolamine-specific phospholipase D activity (GO:0070290), glycerophospholipase activity (GO:0004620), hydrolase activity (GO:0016787), metal ion binding (GO:0046872)

GO Cellular Component (16): Golgi membrane (GO:0000139), nuclear envelope (GO:0005635), nucleoplasm (GO:0005654), cytoplasm (GO:0005737), early endosome (GO:0005769), Golgi apparatus (GO:0005794), smooth endoplasmic reticulum membrane (GO:0030868), early endosome membrane (GO:0031901), photoreceptor outer segment membrane (GO:0042622), presynaptic membrane (GO:0042734), neuron projection (GO:0043005), neuronal cell body (GO:0043025), postsynaptic membrane (GO:0045211), extracellular exosome (GO:0070062), hippocampal mossy fiber to CA3 synapse (GO:0098686), presynapse (GO:0098793)

Reactome top-level categories

4 top-level categories:

Category	Pathways
Retinoid cycle disease events	1
Diseases associated with visual transduction	1
Diseases of the neuronal system	1
Disease	1

GO top-level categories

59 GO namespaces:

Category	Terms
cellular anatomical structure	3
lipid metabolic process	2
bounding membrane of organelle	2
endomembrane system	2
synaptic membrane	2
multicellular organismal-level homeostasis	1
phospholipid metabolic process	1
lipid catabolic process	1
organophosphate catabolic process	1
multicellular organismal response to stress	1
response to alcohol	1
homeostasis of number of cells	1
host-mediated perturbation of symbiont process	1
inflammatory response	1
positive regulation of defense response	1
positive regulation of response to external stimulus	1
regulation of inflammatory response	1
primary alcohol metabolic process	1
phosphatidylethanolamine metabolic process	1
positive regulation of fat cell differentiation	1
brown fat cell differentiation	1
regulation of brown fat cell differentiation	1
eating behavior	1
regulation of eating behavior	1
negative regulation of feeding behavior	1
primary metabolic process	1
organophosphate metabolic process	1
catabolic process	1
transition metal ion binding	1
monocarboxylic acid binding	1
protein binding	1
D-type glycerophospholipase activity	1
phospholipase activity	1
catalytic activity	1
cation binding	1
Golgi apparatus	1
nucleus	1
organelle envelope	1
nuclear lumen	1
intracellular anatomical structure	1
endosome	1
cytoplasm	1
intracellular membrane-bounded organelle	1
endoplasmic reticulum membrane	1
smooth endoplasmic reticulum	1
early endosome	1
endosome membrane	1
photoreceptor outer segment	1
ciliary membrane	1
presynapse	1
plasma membrane bounded cell projection	1
somatodendritic compartment	1
cell body	1
postsynapse	1
extracellular vesicle	1
thorny excrescence	1
neuron to neuron synapse	1
hippocampal mossy fiber expansion	1
synapse	1

Experimentally-supported GO annotations

GO terms backed by direct experimental evidence (ECO experimental codes) — 7 of 36 annotations. The rest are phylogenetic / computational / electronic (IEA).

7 experimentally-supported GO terms:

GO term	NS	Evidence
N-acylphosphatidylethanolamine metabolic process	BP	direct assay
Golgi apparatus	CC	direct assay
extracellular exosome	CC	high-throughput assay
N-acylphosphatidylethanolamine-specific phospholipase D activity	MF	direct assay
bile acid binding	MF	direct assay
identical protein binding	MF	physical interaction
zinc ion binding	MF	direct assay

Protein interactions and networks

STRING

showing 15 of 682 interactions by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
NAPEPLD	FAAH	O00519	923
NAPEPLD	PLD2	O14939	910
NAPEPLD	MGLL	Q99685	907
NAPEPLD	DAGLB	Q8NCG7	905
NAPEPLD	DAGLA	Q9Y4D2	891
NAPEPLD	GDE1	Q9NZC3	848
NAPEPLD	ABHD4	Q8TB40	833
NAPEPLD	ABHD6	Q9BV23	823
NAPEPLD	NAAA	Q02083	808
NAPEPLD	ABHD12	Q8N2K0	781
NAPEPLD	CNR1	P21554	773
NAPEPLD	FAAH2	Q6GMR7	771
NAPEPLD	GPR55	Q9Y2T6	771
NAPEPLD	TRPV1	Q8NER1	731
NAPEPLD	GPR119	Q8TDV5	704

IntAct

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

1 partners by confidence:

Partner	Interaction type	MIscore	Records
DISC1	physical association	0.000	1

BioGRID (5 interactions; top human partners by supporting records): CLEC4M (Affinity Capture-MS), DDX39A (Affinity Capture-RNA), LMBRD1 (Cross-Linking-MS (XL-MS)), NUDT21 (Affinity Capture-RNA), PPP1CC (Two-hybrid)

Disease & clinical

Genetic variants

Variant evidence for NAPEPLD: 78 ClinVar records (1 pathogenic / likely pathogenic). Per-variant detail is on Sugi Variant.

ClinVar

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

Classification	Count (floor)
Pathogenic	1
Likely pathogenic	0
Uncertain significance	58
Likely benign	2
Benign	2

Top pathogenic / likely-pathogenic (1)

Showing all 1 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
4070958	NM_001122838.3(NAPEPLD):c.945G>T (p.Trp315Cys)	Pathogenic	no assertion criteria provided	1

Per-variant reference — Sugi Variant

Explore NAPEPLD’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; 21 predictions of 1,030):

Position(s)	Effect	Δscore	Sites
7:103128597	donor_gain	1.0000
7:103148054	donor_gain	1.0000
7:103103459	donor_gain	0.9900
7:103103561	acceptor_gain	0.9900
7:103117683	donor_gain	0.9900
7:103120228–103120232	acceptor_gain	0.9900	3
7:103128793–103128794	acceptor_loss	0.9900	6
7:103148886	donor_gain	0.9900
7:103103560	acceptor_gain	0.9800
7:103119575–103119576	donor_loss	0.9800	5

AlphaMissense

913 missense substitutions predicted likely pathogenic (of 2,628 scored), across 223 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
D189	8	0.980	0.990
H190	8	0.980	0.992
D147	8	0.976	0.992
H185	8	0.974	0.984
H253	8	0.972	0.987
D284	8	0.971	0.995
H187	8	0.968	0.982
H321	8	0.965	0.983
H343	8	0.956	0.988
D192	8	0.943	0.981
H132	8	0.934	0.973
W232	7	0.988	0.998
W209	7	0.987	0.999
W267	7	0.982	0.998
F347	7	0.970	0.993
W129	7	0.967	0.995
F65	7	0.965	0.990
W270	7	0.965	0.998
W233	7	0.959	0.996
S184	7	0.956	0.999

HPA cancer prognostics

RNA cancer specificity: Low cancer specificity

Human Protein Atlas survival analysis — favorable = higher expression predicts better survival.

3 prognostic cancer types:

Cancer	Prognostic	p-value
Kidney Renal Clear Cell Carcinoma (TCGA)	favorable	3.35e-08
Pancreatic Adenocarcinoma (TCGA)	unfavorable	7.56e-05
Rectum Adenocarcinoma (TCGA)	favorable	0.000954

Disease associations

OMIM: gene MIM:612334 | disease phenotypes: MIM:143890

GenCC curated gene-disease

Mondo (1): hypercholesterolemia, familial, 1 (MONDO:0007750)

Orphanet (1): Homozygous familial hypercholesterolemia (Orphanet:391665)

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL4630839 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

Phase ≥1, by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 26,440 (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
CHEMBL496	HEXACHLOROPHENE	4	26,440

PharmGKB: 1 entry (CPIC guideline: no)

GtoPdb / IUPHAR curated pharmacology

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

Target class: enzyme — N-Acylethanolamine turnover

Most potent curated ligand interactions (8 total), top 8:

Ligand	Action	Affinity	Parameter
LEI-401	Inhibition	7.57	pKi
N3SA	Binding	7.48	pKd
indapamide	Binding	6.24	pKd
chlorthalidone	Binding	6.17	pKd
hydrochlorothiazide	Binding	5.1	pKd
hexachlorophene	Inhibition	5.01	pIC50
bithionol	Inhibition	4.97	pIC50
ARN19874	Inhibition	4.47	pIC50

Binding affinities (BindingDB)

105 measured of 113 human assays (113 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value
CHEMBL4794048	IC50	72 nM
CHEMBL4761882	IC50	110 nM
CHEMBL4782800	IC50	112 nM
CHEMBL4752937	IC50	155 nM
CHEMBL4754918	IC50	209 nM
CHEMBL4751223	IC50	224 nM
CHEMBL4783103	IC50	224 nM
CHEMBL4759968	IC50	234 nM
CHEMBL4760293	IC50	251 nM
CHEMBL4752023	IC50	282 nM
CHEMBL4747615	IC50	288 nM
CHEMBL4764910	IC50	302 nM
CHEMBL4750592	IC50	324 nM
CHEMBL4760794	IC50	380 nM
CHEMBL4752088	IC50	380 nM
CHEMBL4746912	IC50	389 nM
CHEMBL4750134	IC50	407 nM
CHEMBL4795010	IC50	427 nM
CHEMBL4764783	IC50	490 nM
CHEMBL4787774	IC50	501 nM
CHEMBL4743071	IC50	525 nM
CHEMBL4750396	IC50	603 nM
CHEMBL4756143	IC50	646 nM
CHEMBL4741598	IC50	646 nM
CHEMBL4792394	IC50	708 nM
CHEMBL4764562	IC50	741 nM
CHEMBL4787757	IC50	741 nM
CHEMBL4795013	IC50	776 nM
CHEMBL4790197	IC50	813 nM
CHEMBL4747267	IC50	832 nM
CHEMBL4762577	IC50	851 nM
CHEMBL4789858	IC50	891 nM
CHEMBL4795197	IC50	912 nM
CHEMBL4745098	IC50	977 nM
CHEMBL4764089	IC50	1000 nM
CHEMBL4777828	IC50	1000 nM
CHEMBL4750056	IC50	1070 nM
CHEMBL4764340	IC50	1100 nM
CHEMBL4756683	IC50	1100 nM
CHEMBL4751965	IC50	1120 nM
CHEMBL4779869	IC50	1180 nM
CHEMBL4776045	IC50	1200 nM
CHEMBL4757430	IC50	1200 nM
CHEMBL4786525	IC50	1230 nM
SMR000058356	IC50	1300 nM
CHEMBL4749127	IC50	1410 nM
CHEMBL4762175	IC50	1440 nM
CHEMBL4740570	IC50	1580 nM
CHEMBL4740363	IC50	1660 nM
CHEMBL4755036	IC50	1820 nM

ChEMBL bioactivities

82 potent at pChembl≥5 of 106 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
7.14	IC50	72.44	nM	CHEMBL4794048
6.96	IC50	109.7	nM	CHEMBL4761882
6.95	IC50	112.2	nM	CHEMBL4782800
6.81	IC50	154.9	nM	CHEMBL4752937
6.68	IC50	208.9	nM	CHEMBL4754918
6.65	IC50	223.9	nM	CHEMBL4751223
6.65	IC50	223.9	nM	CHEMBL4783103
6.63	IC50	234.4	nM	CHEMBL4759968
6.60	IC50	251.2	nM	CHEMBL4760293
6.55	IC50	281.8	nM	CHEMBL4752023
6.54	IC50	288.4	nM	CHEMBL4747615
6.52	IC50	302	nM	CHEMBL4764910
6.49	IC50	323.6	nM	CHEMBL4750592
6.42	IC50	380.2	nM	CHEMBL4760794
6.42	IC50	380.2	nM	CHEMBL4752088
6.41	IC50	389.1	nM	CHEMBL4746912
6.39	IC50	407.4	nM	CHEMBL4750134
6.37	IC50	426.6	nM	CHEMBL4795010
6.31	IC50	489.8	nM	CHEMBL4764783
6.30	IC50	501.2	nM	CHEMBL4787774
6.28	IC50	524.8	nM	CHEMBL4743071
6.22	IC50	602.6	nM	CHEMBL4750396
6.19	IC50	645.6	nM	CHEMBL4756143
6.19	IC50	645.6	nM	CHEMBL4741598
6.15	IC50	708	nM	CHEMBL4792394
6.13	IC50	741.3	nM	CHEMBL4764562
6.13	IC50	741.3	nM	CHEMBL4787757
6.11	IC50	776.2	nM	CHEMBL4795013
6.09	IC50	812.8	nM	CHEMBL4790197
6.08	IC50	831.8	nM	CHEMBL4747267
6.07	IC50	851.1	nM	CHEMBL4762577
6.05	IC50	891.2	nM	CHEMBL4789858
6.04	IC50	912	nM	CHEMBL4795197
6.01	IC50	977.2	nM	CHEMBL4745098
6.00	IC50	1000	nM	CHEMBL4764089
6.00	IC50	1000	nM	CHEMBL4777828
5.97	IC50	1072	nM	CHEMBL4750056
5.96	IC50	1096	nM	CHEMBL4764340
5.96	IC50	1096	nM	CHEMBL4756683
5.95	IC50	1122	nM	CHEMBL4751965
5.93	IC50	1175	nM	CHEMBL4779869
5.92	IC50	1202	nM	CHEMBL4776045
5.92	IC50	1202	nM	CHEMBL4757430
5.91	IC50	1230	nM	CHEMBL4786525
5.85	IC50	1413	nM	CHEMBL4749127
5.84	IC50	1445	nM	CHEMBL4762175
5.80	IC50	1585	nM	CHEMBL4740570
5.80	IC50	1600	nM	HEXACHLOROPHENE
5.78	IC50	1660	nM	CHEMBL4740363
5.74	IC50	1820	nM	CHEMBL4755036

PubChem BioAssay actives

82 with measured affinity, of 115 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
N-(cyclopropylmethyl)-6-[(3S)-3-hydroxypyrrolidin-1-yl]-2-[(3S)-3-phenylpiperidin-1-yl]pyrimidine-4-carboxamide	1707626: Inhibition of full length human NAPE-PLD expressed in HEK293T cell lysate using PED6 as substrate preincubated for 30 mins followed by substrate addition and measured at 2 mins interval for 1 hr by tecan-plate reader analysis	ic50	0.0724	uM
N-(cyclopropylmethyl)-6-[(3R)-3-hydroxypyrrolidin-1-yl]-2-[(3S)-3-phenylpiperidin-1-yl]pyrimidine-4-carboxamide	1707626: Inhibition of full length human NAPE-PLD expressed in HEK293T cell lysate using PED6 as substrate preincubated for 30 mins followed by substrate addition and measured at 2 mins interval for 1 hr by tecan-plate reader analysis	ic50	0.1096	uM
N-(cyclopropylmethyl)-6-(dimethylamino)-2-[(3S)-3-phenylpiperidin-1-yl]pyrimidine-4-carboxamide	1707626: Inhibition of full length human NAPE-PLD expressed in HEK293T cell lysate using PED6 as substrate preincubated for 30 mins followed by substrate addition and measured at 2 mins interval for 1 hr by tecan-plate reader analysis	ic50	0.1122	uM
N-(cyclopropylmethyl)-2,6-bis[methyl(2-phenylethyl)amino]pyrimidine-4-carboxamide	1707626: Inhibition of full length human NAPE-PLD expressed in HEK293T cell lysate using PED6 as substrate preincubated for 30 mins followed by substrate addition and measured at 2 mins interval for 1 hr by tecan-plate reader analysis	ic50	0.1549	uM
N-(cyclopropylmethyl)-6-morpholin-4-yl-2-[(3S)-3-phenylpiperidin-1-yl]pyrimidine-4-carboxamide	1707626: Inhibition of full length human NAPE-PLD expressed in HEK293T cell lysate using PED6 as substrate preincubated for 30 mins followed by substrate addition and measured at 2 mins interval for 1 hr by tecan-plate reader analysis	ic50	0.2089	uM
N-(cyclopropylmethyl)-6-(3-hydroxypyrrolidin-1-yl)-2-[methyl(2-phenylethyl)amino]pyrimidine-4-carboxamide	1707626: Inhibition of full length human NAPE-PLD expressed in HEK293T cell lysate using PED6 as substrate preincubated for 30 mins followed by substrate addition and measured at 2 mins interval for 1 hr by tecan-plate reader analysis	ic50	0.2239	uM
N-(cyclopropylmethyl)-2-[methyl(2-phenylethyl)amino]-6-pyrrolidin-1-ylpyrimidine-4-carboxamide	1707626: Inhibition of full length human NAPE-PLD expressed in HEK293T cell lysate using PED6 as substrate preincubated for 30 mins followed by substrate addition and measured at 2 mins interval for 1 hr by tecan-plate reader analysis	ic50	0.2239	uM
N-(cyclopropylmethyl)-6-[(3S)-3-hydroxypyrrolidin-1-yl]-2-[methyl(2-phenylethyl)amino]pyrimidine-4-carboxamide	1707626: Inhibition of full length human NAPE-PLD expressed in HEK293T cell lysate using PED6 as substrate preincubated for 30 mins followed by substrate addition and measured at 2 mins interval for 1 hr by tecan-plate reader analysis	ic50	0.2344	uM
N-(cyclopropylmethyl)-6-[(3S)-3-hydroxypyrrolidin-1-yl]-2-[(3R)-3-phenylpiperidin-1-yl]pyrimidine-4-carboxamide	1707626: Inhibition of full length human NAPE-PLD expressed in HEK293T cell lysate using PED6 as substrate preincubated for 30 mins followed by substrate addition and measured at 2 mins interval for 1 hr by tecan-plate reader analysis	ic50	0.2512	uM
N-(cyclopropylmethyl)-6-morpholin-4-yl-2-[2-phenylethyl(propan-2-yl)amino]pyrimidine-4-carboxamide	1707626: Inhibition of full length human NAPE-PLD expressed in HEK293T cell lysate using PED6 as substrate preincubated for 30 mins followed by substrate addition and measured at 2 mins interval for 1 hr by tecan-plate reader analysis	ic50	0.2818	uM
N-(cyclopropylmethyl)-6-(dimethylamino)-2-[methyl(2-phenylethyl)amino]pyrimidine-4-carboxamide	1707626: Inhibition of full length human NAPE-PLD expressed in HEK293T cell lysate using PED6 as substrate preincubated for 30 mins followed by substrate addition and measured at 2 mins interval for 1 hr by tecan-plate reader analysis	ic50	0.2884	uM
N-(cyclopropylmethyl)-6-[(3R)-3-hydroxypyrrolidin-1-yl]-2-[methyl(2-phenylethyl)amino]pyrimidine-4-carboxamide	1707626: Inhibition of full length human NAPE-PLD expressed in HEK293T cell lysate using PED6 as substrate preincubated for 30 mins followed by substrate addition and measured at 2 mins interval for 1 hr by tecan-plate reader analysis	ic50	0.3020	uM
N-(cyclopropylmethyl)-6-[(3R)-3-hydroxypyrrolidin-1-yl]-2-[(3R)-3-phenylpiperidin-1-yl]pyrimidine-4-carboxamide	1707626: Inhibition of full length human NAPE-PLD expressed in HEK293T cell lysate using PED6 as substrate preincubated for 30 mins followed by substrate addition and measured at 2 mins interval for 1 hr by tecan-plate reader analysis	ic50	0.3236	uM
N-(cyclopropylmethyl)-6-morpholin-4-yl-2-(3-phenylpiperidin-1-yl)pyrimidine-4-carboxamide	1707626: Inhibition of full length human NAPE-PLD expressed in HEK293T cell lysate using PED6 as substrate preincubated for 30 mins followed by substrate addition and measured at 2 mins interval for 1 hr by tecan-plate reader analysis	ic50	0.3802	uM
2-(2-benzylpyrrolidin-1-yl)-N-(cyclopropylmethyl)-6-morpholin-4-ylpyrimidine-4-carboxamide	1707626: Inhibition of full length human NAPE-PLD expressed in HEK293T cell lysate using PED6 as substrate preincubated for 30 mins followed by substrate addition and measured at 2 mins interval for 1 hr by tecan-plate reader analysis	ic50	0.3802	uM
N-(cyclopropylmethyl)-6-(3,3-difluoropiperidin-1-yl)-2-[methyl(2-phenylethyl)amino]pyrimidine-4-carboxamide	1707626: Inhibition of full length human NAPE-PLD expressed in HEK293T cell lysate using PED6 as substrate preincubated for 30 mins followed by substrate addition and measured at 2 mins interval for 1 hr by tecan-plate reader analysis	ic50	0.3891	uM
N-(cyclopropylmethyl)-6-(dimethylamino)-2-[(3R)-3-phenylpiperidin-1-yl]pyrimidine-4-carboxamide	1707626: Inhibition of full length human NAPE-PLD expressed in HEK293T cell lysate using PED6 as substrate preincubated for 30 mins followed by substrate addition and measured at 2 mins interval for 1 hr by tecan-plate reader analysis	ic50	0.4074	uM
6-(azetidin-1-yl)-N-(cyclopropylmethyl)-2-[methyl(2-phenylethyl)amino]pyrimidine-4-carboxamide	1707626: Inhibition of full length human NAPE-PLD expressed in HEK293T cell lysate using PED6 as substrate preincubated for 30 mins followed by substrate addition and measured at 2 mins interval for 1 hr by tecan-plate reader analysis	ic50	0.4266	uM
N-(cyclopropylmethyl)-2-[methyl-[2-(2-phenylphenyl)ethyl]amino]-6-morpholin-4-ylpyrimidine-4-carboxamide	1707626: Inhibition of full length human NAPE-PLD expressed in HEK293T cell lysate using PED6 as substrate preincubated for 30 mins followed by substrate addition and measured at 2 mins interval for 1 hr by tecan-plate reader analysis	ic50	0.4898	uM
N-(cyclopropylmethyl)-6-(diethylamino)-2-[methyl(2-phenylethyl)amino]pyrimidine-4-carboxamide	1707626: Inhibition of full length human NAPE-PLD expressed in HEK293T cell lysate using PED6 as substrate preincubated for 30 mins followed by substrate addition and measured at 2 mins interval for 1 hr by tecan-plate reader analysis	ic50	0.5012	uM
2-[bis(2-phenylethyl)amino]-N-(cyclopropylmethyl)-6-morpholin-4-ylpyrimidine-4-carboxamide	1707626: Inhibition of full length human NAPE-PLD expressed in HEK293T cell lysate using PED6 as substrate preincubated for 30 mins followed by substrate addition and measured at 2 mins interval for 1 hr by tecan-plate reader analysis	ic50	0.5248	uM
N-(cyclopropylmethyl)-2-[methyl-[2-(2-phenoxyphenyl)ethyl]amino]-6-morpholin-4-ylpyrimidine-4-carboxamide	1707626: Inhibition of full length human NAPE-PLD expressed in HEK293T cell lysate using PED6 as substrate preincubated for 30 mins followed by substrate addition and measured at 2 mins interval for 1 hr by tecan-plate reader analysis	ic50	0.6026	uM
N-(cyclopropylmethyl)-2-[ethyl(2-phenylethyl)amino]-6-morpholin-4-ylpyrimidine-4-carboxamide	1707626: Inhibition of full length human NAPE-PLD expressed in HEK293T cell lysate using PED6 as substrate preincubated for 30 mins followed by substrate addition and measured at 2 mins interval for 1 hr by tecan-plate reader analysis	ic50	0.6456	uM
N-(cyclopropylmethyl)-2-[methyl(2-phenylethyl)amino]-6-piperidin-1-ylpyrimidine-4-carboxamide	1707626: Inhibition of full length human NAPE-PLD expressed in HEK293T cell lysate using PED6 as substrate preincubated for 30 mins followed by substrate addition and measured at 2 mins interval for 1 hr by tecan-plate reader analysis	ic50	0.6456	uM
N-(cyclopropylmethyl)-6-(3-methoxypyrrolidin-1-yl)-2-[methyl(2-phenylethyl)amino]pyrimidine-4-carboxamide	1707626: Inhibition of full length human NAPE-PLD expressed in HEK293T cell lysate using PED6 as substrate preincubated for 30 mins followed by substrate addition and measured at 2 mins interval for 1 hr by tecan-plate reader analysis	ic50	0.7079	uM
2-[benzyl(2-phenylethyl)amino]-N-(cyclopropylmethyl)-6-morpholin-4-ylpyrimidine-4-carboxamide	1707626: Inhibition of full length human NAPE-PLD expressed in HEK293T cell lysate using PED6 as substrate preincubated for 30 mins followed by substrate addition and measured at 2 mins interval for 1 hr by tecan-plate reader analysis	ic50	0.7413	uM
2-(2-benzylpiperidin-1-yl)-N-(cyclopropylmethyl)-6-morpholin-4-ylpyrimidine-4-carboxamide	1707626: Inhibition of full length human NAPE-PLD expressed in HEK293T cell lysate using PED6 as substrate preincubated for 30 mins followed by substrate addition and measured at 2 mins interval for 1 hr by tecan-plate reader analysis	ic50	0.7413	uM
N-(cyclopropylmethyl)-2-[2-(2-methoxyphenyl)ethyl-methylamino]-6-morpholin-4-ylpyrimidine-4-carboxamide	1707626: Inhibition of full length human NAPE-PLD expressed in HEK293T cell lysate using PED6 as substrate preincubated for 30 mins followed by substrate addition and measured at 2 mins interval for 1 hr by tecan-plate reader analysis	ic50	0.7762	uM
N-(cyclopropylmethyl)-2-[methyl(2-phenylethyl)amino]-6-morpholin-4-ylpyrimidine-4-carboxamide	1707626: Inhibition of full length human NAPE-PLD expressed in HEK293T cell lysate using PED6 as substrate preincubated for 30 mins followed by substrate addition and measured at 2 mins interval for 1 hr by tecan-plate reader analysis	ic50	0.8128	uM
methyl 2-[[2-[methyl(2-phenylethyl)amino]-6-morpholin-4-ylpyrimidine-4-carbonyl]amino]acetate	1707626: Inhibition of full length human NAPE-PLD expressed in HEK293T cell lysate using PED6 as substrate preincubated for 30 mins followed by substrate addition and measured at 2 mins interval for 1 hr by tecan-plate reader analysis	ic50	0.8318	uM
N-(cyclopropylmethyl)-6-(methylamino)-2-[methyl(2-phenylethyl)amino]pyrimidine-4-carboxamide	1707626: Inhibition of full length human NAPE-PLD expressed in HEK293T cell lysate using PED6 as substrate preincubated for 30 mins followed by substrate addition and measured at 2 mins interval for 1 hr by tecan-plate reader analysis	ic50	0.8511	uM
N-(cyclopropylmethyl)-2-[methyl-[2-(2-methylphenyl)ethyl]amino]-6-morpholin-4-ylpyrimidine-4-carboxamide	1707626: Inhibition of full length human NAPE-PLD expressed in HEK293T cell lysate using PED6 as substrate preincubated for 30 mins followed by substrate addition and measured at 2 mins interval for 1 hr by tecan-plate reader analysis	ic50	0.8912	uM
2-[methyl(2-phenylethyl)amino]-6-morpholin-4-yl-N-prop-2-ynylpyrimidine-4-carboxamide	1707626: Inhibition of full length human NAPE-PLD expressed in HEK293T cell lysate using PED6 as substrate preincubated for 30 mins followed by substrate addition and measured at 2 mins interval for 1 hr by tecan-plate reader analysis	ic50	0.9120	uM
2-[2-(2-chlorophenyl)ethyl-methylamino]-N-(cyclopropylmethyl)-6-morpholin-4-ylpyrimidine-4-carboxamide	1707626: Inhibition of full length human NAPE-PLD expressed in HEK293T cell lysate using PED6 as substrate preincubated for 30 mins followed by substrate addition and measured at 2 mins interval for 1 hr by tecan-plate reader analysis	ic50	0.9772	uM
2-(4-benzyl-3-phenylpiperazin-1-yl)-N-(cyclopropylmethyl)-6-morpholin-4-ylpyrimidine-4-carboxamide	1707626: Inhibition of full length human NAPE-PLD expressed in HEK293T cell lysate using PED6 as substrate preincubated for 30 mins followed by substrate addition and measured at 2 mins interval for 1 hr by tecan-plate reader analysis	ic50	1.0000	uM
N-(cyclopropylmethyl)-6-[2-hydroxyethyl(methyl)amino]-2-[methyl(2-phenylethyl)amino]pyrimidine-4-carboxamide	1707626: Inhibition of full length human NAPE-PLD expressed in HEK293T cell lysate using PED6 as substrate preincubated for 30 mins followed by substrate addition and measured at 2 mins interval for 1 hr by tecan-plate reader analysis	ic50	1.0000	uM
N-(cyclopropylmethyl)-2-[methyl(2-thiophen-2-ylethyl)amino]-6-morpholin-4-ylpyrimidine-4-carboxamide	1707626: Inhibition of full length human NAPE-PLD expressed in HEK293T cell lysate using PED6 as substrate preincubated for 30 mins followed by substrate addition and measured at 2 mins interval for 1 hr by tecan-plate reader analysis	ic50	1.0715	uM
N-(cyclopropylmethyl)-2-[cyclopropyl(2-phenylethyl)amino]-6-morpholin-4-ylpyrimidine-4-carboxamide	1707626: Inhibition of full length human NAPE-PLD expressed in HEK293T cell lysate using PED6 as substrate preincubated for 30 mins followed by substrate addition and measured at 2 mins interval for 1 hr by tecan-plate reader analysis	ic50	1.0965	uM
6-[benzyl(methyl)amino]-N-(cyclopropylmethyl)-2-[methyl(2-phenylethyl)amino]pyrimidine-4-carboxamide	1707626: Inhibition of full length human NAPE-PLD expressed in HEK293T cell lysate using PED6 as substrate preincubated for 30 mins followed by substrate addition and measured at 2 mins interval for 1 hr by tecan-plate reader analysis	ic50	1.0965	uM
N-(cyclopropylmethyl)-6-morpholin-4-yl-2-[N-(2-phenylethyl)anilino]pyrimidine-4-carboxamide	1707626: Inhibition of full length human NAPE-PLD expressed in HEK293T cell lysate using PED6 as substrate preincubated for 30 mins followed by substrate addition and measured at 2 mins interval for 1 hr by tecan-plate reader analysis	ic50	1.1220	uM
N-(cyclopropylmethyl)-6-(3,3-difluoropyrrolidin-1-yl)-2-[methyl(2-phenylethyl)amino]pyrimidine-4-carboxamide	1707626: Inhibition of full length human NAPE-PLD expressed in HEK293T cell lysate using PED6 as substrate preincubated for 30 mins followed by substrate addition and measured at 2 mins interval for 1 hr by tecan-plate reader analysis	ic50	1.1749	uM
6-(4-acetylpiperazin-1-yl)-N-(cyclopropylmethyl)-2-[methyl(2-phenylethyl)amino]pyrimidine-4-carboxamide	1707626: Inhibition of full length human NAPE-PLD expressed in HEK293T cell lysate using PED6 as substrate preincubated for 30 mins followed by substrate addition and measured at 2 mins interval for 1 hr by tecan-plate reader analysis	ic50	1.2023	uM
N-(cyclopropylmethyl)-2-[methyl(2-phenylethyl)amino]-6-pyrazol-1-ylpyrimidine-4-carboxamide	1707626: Inhibition of full length human NAPE-PLD expressed in HEK293T cell lysate using PED6 as substrate preincubated for 30 mins followed by substrate addition and measured at 2 mins interval for 1 hr by tecan-plate reader analysis	ic50	1.2023	uM
N-(cyclopropylmethyl)-6-morpholin-4-yl-2-(2-phenylmorpholin-4-yl)pyrimidine-4-carboxamide	1707626: Inhibition of full length human NAPE-PLD expressed in HEK293T cell lysate using PED6 as substrate preincubated for 30 mins followed by substrate addition and measured at 2 mins interval for 1 hr by tecan-plate reader analysis	ic50	1.2303	uM
N-(cyclopropylmethyl)-2-[methyl(2-phenylethyl)amino]-6-(3-phenylpyrrolidin-1-yl)pyrimidine-4-carboxamide	1707626: Inhibition of full length human NAPE-PLD expressed in HEK293T cell lysate using PED6 as substrate preincubated for 30 mins followed by substrate addition and measured at 2 mins interval for 1 hr by tecan-plate reader analysis	ic50	1.4125	uM
N-(cyclopropylmethyl)-2-[methyl(2-phenylethyl)amino]-6-morpholin-4-ylpyridine-4-carboxamide	1707626: Inhibition of full length human NAPE-PLD expressed in HEK293T cell lysate using PED6 as substrate preincubated for 30 mins followed by substrate addition and measured at 2 mins interval for 1 hr by tecan-plate reader analysis	ic50	1.4454	uM
N-(cyclopropylmethyl)-2-[methyl(2-phenylethyl)amino]-6-(4-methylpiperazin-1-yl)pyrimidine-4-carboxamide	1707626: Inhibition of full length human NAPE-PLD expressed in HEK293T cell lysate using PED6 as substrate preincubated for 30 mins followed by substrate addition and measured at 2 mins interval for 1 hr by tecan-plate reader analysis	ic50	1.5849	uM
3,4,6-trichloro-2-[(2,3,5-trichloro-6-hydroxyphenyl)methyl]phenol	1707626: Inhibition of full length human NAPE-PLD expressed in HEK293T cell lysate using PED6 as substrate preincubated for 30 mins followed by substrate addition and measured at 2 mins interval for 1 hr by tecan-plate reader analysis	ic50	1.6000	uM
N-(cyclopropylmethyl)-2-[methyl(2-phenylethyl)amino]-6-(2-oxa-6-azaspiro[3.3]heptan-6-yl)pyrimidine-4-carboxamide	1707626: Inhibition of full length human NAPE-PLD expressed in HEK293T cell lysate using PED6 as substrate preincubated for 30 mins followed by substrate addition and measured at 2 mins interval for 1 hr by tecan-plate reader analysis	ic50	1.6596	uM
2-[methyl(2-phenylethyl)amino]-6-morpholin-4-yl-N-propylpyrimidine-4-carboxamide	1707626: Inhibition of full length human NAPE-PLD expressed in HEK293T cell lysate using PED6 as substrate preincubated for 30 mins followed by substrate addition and measured at 2 mins interval for 1 hr by tecan-plate reader analysis	ic50	1.8197	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
Valproic Acid	affects expression, increases expression	3
potassium chromate(VI)	decreases expression, affects cotreatment	2
Dronabinol	affects expression, decreases expression	2
Tobacco Smoke Pollution	decreases expression	2
Cyclosporine	decreases expression	2
Cadmium Chloride	decreases expression, increases expression	2
methylmercuric chloride	decreases expression	1
triphenyl phosphate	affects expression	1
cannabichromene	decreases expression, increases expression	1
trichostatin A	increases expression	1
tris(2-butoxyethyl) phosphate	affects expression	1
beta-lapachone	decreases expression	1
tris(1,3-dichloro-2-propyl)phosphate	decreases expression	1
sodium arsenite	decreases expression	1
butyraldehyde	decreases expression	1
epigallocatechin gallate	affects cotreatment, decreases expression	1
di-n-butylphosphoric acid	affects expression	1
chromium hexavalent ion	decreases expression	1
perfluoro-n-nonanoic acid	decreases expression	1
Temozolomide	decreases expression	1
Zoledronic Acid	increases expression	1
Acetaminophen	decreases expression	1
Air Pollutants	decreases expression, increases abundance	1
Air Pollutants, Occupational	decreases expression	1
Benzo(a)pyrene	increases methylation	1
Cannabidiol	increases expression	1
Cannabinol	decreases expression	1
Carbamazepine	affects expression	1
Diclofenac	affects expression	1
Gold	decreases expression	1

ChEMBL screening assays

3 unique, capped per target: 3 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL4626925	Binding	Inhibition of full length human NAPE-PLD expressed in HEK293T cells assessed as enzyme remaining activity at 10 uM using PED6 as substrate preincubated for 30 mins followed by substrate addition and measured for 1 hr at 2 mins relative to c	Structure-Activity Relationship Studies of α-Ketoamides as Inhibitors of the Phospholipase A and Acyltransferase Enzyme Family. — *J Med Chem*

Clinical trials (associated diseases)

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

28 trials:

NCT	Phase	Status	Title
NCT06231459	Phase 4	COMPLETED	Expression of Pro- and Anti-inflammatory Cytokines During Anti-PCSK9 in Familial Hypercholesterolemia
NCT00000594	Phase 3	COMPLETED	NHLBI Type II Coronary Intervention Study
NCT00092833	Phase 3	TERMINATED	Investigational Drug in Patients With Hypercholesterolemia or in Patients With Sitosterolemia (0653-026)(COMPLETED)
NCT00134485	Phase 3	COMPLETED	Study To Evaluate The Safety And Efficacy Of Torcetrapib/Atorvastatin In Subjects With Familial Hypercholerolemia
NCT00134511	Phase 3	COMPLETED	Study To Evaluate The Effect Of Torcetrapib/Atorvastatin In Patients With Genetic High Cholesterol Disorder
NCT00136981	Phase 3	COMPLETED	Carotid B-Mode Ultrasound Study to Compare Anti-Atherosclerotic Effect of Torcetrpib/Atorvastatin to Atorvastatin Alone.
NCT00384293	Phase 3	TERMINATED	Carotid IMT (Intima Media Thickening) Study (0524A-041)(TERMINATED)
NCT01524289	Phase 3	COMPLETED	Study to Assess the Tolerability and Efficacy of Anacetrapib (MK-0859) Co-Administered With Statin in Participants With Heterozygous Familial Hypercholesterolemia (MK-0859-020)
NCT00280995	Phase 2	COMPLETED	Dose-escalating Safety Study of ISIS 301012 in Homozygous Familial Hypercholesterolemia Subjects on Lipid Lowering Therapy
NCT00281008	Phase 2	COMPLETED	Study of ISIS 301012 (Mipomersen) in Heterozygous Familial Hypercholesterolemia Subjects on Lipid Lowering Therapy
NCT01375751	Phase 2	COMPLETED	Reduction of Low-Density Lipoprotein Cholesterol (LDL-C) With PCSK9 Inhibition in Heterozygous Familial Hypercholesterolemia Disorder Study
NCT00515307	Phase 1	COMPLETED	Bone Marrow Stem Cells as a Source of Allogenic Hepatocyte Transplantation in Homozygous Familial Hypercholesterolemia
NCT01583647	Phase 1	TERMINATED	A Study of Extended-release (ER) Niacin/Laropiprant in Adolescents With Heterozygous Familial Hypercholesterolemia (MK-0524A-158)
NCT00005168	Not specified	COMPLETED	Hyperapo B and Coronary Heart Disease
NCT01753232	Not specified	COMPLETED	Safety and Efficacy of the DALI LDL-adsorber and MONET Lipoprotein Filter
NCT03018678	Not specified	COMPLETED	Screening Protocol for a Gene Therapy Trial in Subjects With Homozygous Familial Hypercholesterolemia
NCT03110432	Not specified	COMPLETED	Prospective German Very High Cardiovascular Risk Patients Dyslipidemia Treatment Indication Registry
NCT03795038	Not specified	COMPLETED	Comparison of the Plasma Lipoprotein Apheresis Systems DIAMED and MONET vs. the Whole Blood Apheresis System DALI
NCT03989167	Not specified	RECRUITING	Clinical Decision Support for Familial Hypercholesterolemia
NCT04073797	Not specified	UNKNOWN	PET Imaging of Inflammation and Lipid Lowering Study
NCT04118348	Not specified	COMPLETED	Evaluating the Efficacy of Pediatric Lipid Screening Alerts
NCT04313270	Not specified	UNKNOWN	Subclinical Atherosclerosis in Patients With Familial Hypercholesterolemia Treated With Evolocumab®
NCT04526457	Not specified	COMPLETED	Is Family Screening Improved by Genetic Testing of Familial Hypercholesterolemia
NCT04656028	Not specified	ACTIVE_NOT_RECRUITING	Genetic Testing and Motivational Counseling for FH
NCT04722068	Not specified	COMPLETED	Regeneron 1331 Kinetics Sub-Study HoFH
NCT04837638	Not specified	UNKNOWN	Diet Quality and Coronary Artery Calcification in Adults With Heterozygous Familial Hypercholesterolemia
NCT06555120	Not specified	RECRUITING	Screening for Familial Hypercholesterolemia in Children
NCT07543731	Not specified	RECRUITING	A Real-World Study of Long-Term Adherence and Persistence to Inclisiran, Evolocumab, and Alirocumab

Predicted chemistry — Sugi Predict

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